Page last updated: 2024-12-06

tocophersolan

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Occurs in Manufacturing Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Tocophersolan is a synthetic vitamin E analog with potential therapeutic applications. It is a water-soluble derivative of alpha-tocopherol, the most common form of vitamin E. Tocophersolan is synthesized by attaching a water-soluble moiety, typically a polyethylene glycol (PEG) chain, to the alpha-tocopherol molecule. Research suggests that tocophersolan exhibits antioxidant properties, potentially protecting cells from damage caused by reactive oxygen species. Its water solubility allows for improved bioavailability compared to alpha-tocopherol, enhancing its potential therapeutic benefits. Studies are exploring tocophersolan's efficacy in various conditions, including cardiovascular disease, neurodegenerative disorders, and cancer. The unique properties of tocophersolan, such as its water solubility and antioxidant activity, make it a promising candidate for further investigation in drug development.'

tocophersolan: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71406
CHEBI ID176233
SCHEMBL ID3139787
MeSH IDM0062589

Synonyms (25)

Synonym
CHEBI:176233
1-o-(2-hydroxyethyl) 4-o-[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydrochromen-6-yl] butanedioate
tocophersolan (usan)
D06174
tocofersolan (inn)
vitamin e tpgs
tocophersolan
tocophersolan [usan]
tpgs
tocofersolano
tocofersolanum
tocofersolan [inn]
AKOS015967005
FT-0675259
SCHEMBL3139787
1-(2-hydroxyethyl) 2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydro-2h-1-benzopyran-6-yl butanedioate
30999-06-5
aquasol e tpgs liquid 77iu/ml
tocofersolan, inn
tocophersolan, usan
AOBORMOPSGHCAX-UHFFFAOYSA-N
BCP11679
Q172409
DTXSID50860035
2-hydroxyethyl 2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydro-2h-1-benzopyran-6-yl butanedioate

Research Excerpts

Effects

ExcerptReferenceRelevance
"Tocophersolan has attracted enormous attention as a versatile excipient in different biomedical applications including drug delivery systems and nutraceuticals."( Rediscovering Tocophersolan: A Renaissance for Nano-Based Drug Delivery and Nanotheranostic Applications.
Chen, S; Cui, Q; Wande, DP; Xiong, H; Xu, C; Yao, J, 2021
)
1.7

Toxicity

ExcerptReferenceRelevance
" Results of acute toxicity showed the LD50 of paclitaxel nanosuspensions was 98."( Paclitaxel nanosuspensions coated with P-gp inhibitory surfactants: I. Acute toxicity and pharmacokinetics studies.
Gao, L; Kang, J; Liu, G; Ma, J; Niu, M; Wang, H; Wang, X; Wang, Z, 2013
)
0.39
" This TPGS-based pH-sensitive prodrug provides a safe and "Molecular economical" way in the rational design of prodrugs for overcoming multidrug resistance and targeting delivery, which can improve the potency for clinical use."( A safe, simple and efficient doxorubicin prodrug hybrid micelle for overcoming tumor multidrug resistance and targeting delivery.
Bao, Y; Guo, Y; Hu, X; Sun, Y; Tan, S; Yin, M; Zhang, Z; Zhuang, X, 2016
)
0.43
"Superparamagnetic iron oxide nanoparticles (SPION) require stable surface modifications to render safe nanocapsules for biomedical applications."( Genotoxicity and biocompatibility of superparamagnetic iron oxide nanoparticles: Influence of surface modification on biodistribution, retention, DNA damage and oxidative stress.
Chakrabarti, M; Ghosh, I; Ghosh, S; Mukherjee, A, 2020
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetics and biodistribution results of CUR-NS after intravenous administration in rabbits and mice showed that CUR-NS presented a markedly different pharmacokinetic property as compared to the CUR solution."( Preparation, characterization, pharmacokinetics, and tissue distribution of curcumin nanosuspension with TPGS as stabilizer.
Cao, F; Cui, J; Gao, Y; Guo, C; Li, A; Li, H; Li, Z; Lou, H; Sun, M; Xi, Y; Zhai, G, 2010
)
0.36
" After intravenous injection paclitaxel nanosuspensions displayed different pharmacokinetic properties in comparison with the marketed injectable solution, including a decreased initial drug concentration, increased plasma half-life, AUC and MRT."( Paclitaxel nanosuspensions coated with P-gp inhibitory surfactants: I. Acute toxicity and pharmacokinetics studies.
Gao, L; Kang, J; Liu, G; Ma, J; Niu, M; Wang, H; Wang, X; Wang, Z, 2013
)
0.39
"The paclitaxel nanosuspensions prepared in this study could markedly enhance the tolerance dosage in mice, and manifest different pharmacokinetic properties compared with the solution."( Paclitaxel nanosuspensions coated with P-gp inhibitory surfactants: I. Acute toxicity and pharmacokinetics studies.
Gao, L; Kang, J; Liu, G; Ma, J; Niu, M; Wang, H; Wang, X; Wang, Z, 2013
)
0.39
" Thus, the outcome indicates that RSV-TPGS-Lipo 2 is a promising carrier for glioma treatment with improved pharmacokinetic parameters."( Pharmacokinetics, biodistribution, in vitro cytotoxicity and biocompatibility of Vitamin E TPGS coated trans resveratrol liposomes.
Balavigneswaran, CK; Mahto, SK; Mishra, N; Muthu, MS; Singh, S; Vajanthri, KY; Vijayakumar, MR, 2016
)
0.43
" The pharmacokinetic studies indicated ARS-TPGS-Lipo had higher AUC, longer circulation time and better liver targeting."( The characterization, pharmacokinetic, and tissue distribution studies of TPGS-modified artesunate liposome in rats.
An, R; Hu, C; Liang, K; Wang, X; You, L, 2018
)
0.48
" The pharmacokinetic results in rats showed 50."( Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies.
Mundada, V; Patel, M; Sawant, K, 2019
)
0.51
"23 times greater in Sprague-Dawley male rats compared to marketed formulation, according to in vivo pharmacokinetic data."( Bioavailability enhancement of vitamin E TPGS liposomes of nintedanib esylate: formulation optimization, cytotoxicity and pharmacokinetic studies.
Chinni, S; Kala, SG, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" In combination with an increased throughput (up to 300%) and a reduced animal use (up to 50%), the enhanced power of the differential approach improves the utility of the biorelevant in situ perfusion technique with mesenteric blood sampling to elucidate the intestinal interaction profile of drugs and drug candidates."( Validation of a differential in situ perfusion method with mesenteric blood sampling in rats for intestinal drug interaction profiling.
Annaert, P; Augustijns, P; Brouwers, J; Mols, R, 2010
)
0.36
"Heparin sodium (HS)-loaded polylactic-co-glycolic acid-D-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) nanoparticles (HPTNs) were prepared as a sustained and targeting delivery carrier and combined with emodin (EMO)-loaded PLGA-TPGS nanoparticles (EPTNs), which were investigated previously to form a combination therapy system for the treatment of liver cancer."( Emodin-Loaded PLGA-TPGS Nanoparticles Combined with Heparin Sodium-Loaded PLGA-TPGS Nanoparticles to Enhance Chemotherapeutic Efficacy Against Liver Cancer.
Deng, S; Gao, D; Gao, M; Gao, X; Liu, H; Lv, L; Ma, C; Tian, Y; Wang, C; Xu, H; Zhang, C, 2016
)
0.43
" The apoptosis of HepG2 cells induced by EPTNs in combination with HPTNs was determined by Annexin V-FITC staining and PI labelling."( Emodin-Loaded PLGA-TPGS Nanoparticles Combined with Heparin Sodium-Loaded PLGA-TPGS Nanoparticles to Enhance Chemotherapeutic Efficacy Against Liver Cancer.
Deng, S; Gao, D; Gao, M; Gao, X; Liu, H; Lv, L; Ma, C; Tian, Y; Wang, C; Xu, H; Zhang, C, 2016
)
0.43
" EPTNs combined with HPTNs induced HepG2 cell apoptosis with synergistic effects."( Emodin-Loaded PLGA-TPGS Nanoparticles Combined with Heparin Sodium-Loaded PLGA-TPGS Nanoparticles to Enhance Chemotherapeutic Efficacy Against Liver Cancer.
Deng, S; Gao, D; Gao, M; Gao, X; Liu, H; Lv, L; Ma, C; Tian, Y; Wang, C; Xu, H; Zhang, C, 2016
)
0.43
"Heparin sodium (HS)-loaded polylactic-co-glycolic acid-D-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) nanoparticles (HPTNs) were prepared as sustained and targeted delivery carriers and combined with oleanolic acid (OA)-loaded PLGA-TPGS nanoparticles (OPTNs) that had been investigated in our previous work to form a combination therapy system for the treatment of liver cancer."( Oleanolic acid-loaded PLGA-TPGS nanoparticles combined with heparin sodium-loaded PLGA-TPGS nanoparticles for enhancing chemotherapy to liver cancer.
Bao, X; Deng, S; Gao, D; Gao, M; Guan, X; Liu, H; Lv, L; Tian, Y; Wang, C; Xu, H; Zhang, C, 2016
)
0.43
" The apoptosis of HepG2 cells induced by OPTNs combined with HPTNs was determined by Annexin V-FITC staining and PI labelling."( Oleanolic acid-loaded PLGA-TPGS nanoparticles combined with heparin sodium-loaded PLGA-TPGS nanoparticles for enhancing chemotherapy to liver cancer.
Bao, X; Deng, S; Gao, D; Gao, M; Guan, X; Liu, H; Lv, L; Tian, Y; Wang, C; Xu, H; Zhang, C, 2016
)
0.43
" The cell apoptosis results indicated that OPTNs combined with HPTNs could induce HepG2 cell apoptosis and exert synergistic effects."( Oleanolic acid-loaded PLGA-TPGS nanoparticles combined with heparin sodium-loaded PLGA-TPGS nanoparticles for enhancing chemotherapy to liver cancer.
Bao, X; Deng, S; Gao, D; Gao, M; Guan, X; Liu, H; Lv, L; Tian, Y; Wang, C; Xu, H; Zhang, C, 2016
)
0.43

Bioavailability

Tocophersolan has been widely used for improving the bioavailability of numerous pharmaceutical active ingredients. The present investigation highlights the development of D-α-Tocopheryl polyethylene glycol 1000 succinate.

ExcerptReferenceRelevance
" For the TPGS, a water-soluble form of vitamin E, the indices of bioavailability were lower (P less than ."( Bioavailability of vitamin E compounds in lambs.
Antapli, M; Hidiroglou, N; McDowell, LR; Papas, AM; Wilkinson, NS, 1992
)
0.28
"Twenty-five yearling wethers, weighing 45 to 50 kg, were used in a trial designed to compare the bioavailability of dl-alpha-tocopheryl acetate (TA) and d-alpha-tocopheryl polyethylene glycol-1000 succinate (TPGS)."( Plasma alpha-tocopherol profiles in sheep after oral administration of dl-alpha-tocopheryl acetate and d-alpha-tocopheryl polyethylene glycol-1000 succinate.
Hidiroglou, M; Ivan, M, 1991
)
0.28
" The results of oral vitamin E tolerance tests showed that TPGS was well absorbed in virtually all study subjects, that TPGS intestinal absorption was superior to that of dl-alpha-tocopherol, and that TPGS absorption in teenage children with chronic cholestasis was similar to that of normal adults."( Treatment of vitamin E deficiency during chronic childhood cholestasis with oral d-alpha-tocopheryl polyethylene glycol-1000 succinate.
Butler-Simon, N; Heubi, JE; Lilly, JR; McClung, HJ; Silverman, A; Sokol, RJ, 1987
)
0.27
" D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) is a water-soluble investigational form of vitamin E that is well absorbed during cholestasis."( Tocopheryl polyethylene glycol 1000 succinate therapy for vitamin E deficiency during chronic childhood cholestasis: neurologic outcome.
Bettis, D; Butler-Simon, NA; Silverman, A; Smith, DJ; Sokol, RJ, 1987
)
0.27
" The data also showed that the bioavailability of alpha-tocopherol is dependent on the form administered."( Serum total cholesterol, high-density lipoprotein-cholesterol and triglyceride concentrations in lambs following supplementation with various forms of tocopherol.
Antapli, M; Hidiroglou, N; McDowell, LR; Papas, AM; Wilkinson, NS; Wolynetz, MS, 1993
)
0.29
" These results suggest that enhanced oral bioavailability of drugs co-administered with TPGS may, in part, be due to inhibition of P-glycoprotein in the intestine."( Inhibition of P-glycoprotein by D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS).
Dintaman, JM; Silverman, JA, 1999
)
0.3
"The contributions of cytochrome P450 3A (CYP3A) and P-glycoprotein to sirolimus oral bioavailability in rats were evaluated by coadministration of sirolimus (Rapamune) with the CYP3A inhibitor ketoconazole or the P-glycoprotein inhibitor D-alpha-tocopheryl poly(ethylene glycol 1000) succinate (TPGS)."( Sirolimus oral absorption in rats is increased by ketoconazole but is not affected by D-alpha-tocopheryl poly(ethylene glycol 1000) succinate.
Chai, A; Chan, AO; O'Mahony, D; Ramtoola, Z; Silverman, JA; Tran-Tau, P; Wacher, VJ; Wong, S; Yu, XQ, 2002
)
0.31
"Two surface-active formulation ingredients, a water-soluble derivative of vitamin E (D-alpha-tocopherol polyethylene glycol 1000 succinate, vitamin E-TPGS) as well as a polyethoxylated derivative of 12-hydroxy-stearic acid (Solutol HS 15) were investigated in rats for their potential to increase the oral bioavailability of the p-glycoprotein (p-gp) and cytochrome P450 substrate colchicine."( Improvement of the bioavailability of colchicine in rats by co-administration of D-alpha-tocopherol polyethylene glycol 1000 succinate and a polyethoxylated derivative of 12-hydroxy-stearic acid.
Bittner, B; Fullhardt, P; González, RC; Guenzi, A; Mountfield, RJ; Zuercher, G, 2002
)
0.31
" It is water soluble, having a high molecular weight, and poorly absorbed from the gastrointestinal tract."( Enhanced intestinal absorption of vancomycin with Labrasol and D-alpha-tocopheryl PEG 1000 succinate in rats.
Eaimtrakarn, S; Ishida, M; Prasad, YV; Puthli, SP; Shibata, N; Takada, K; Yoshikawa, Y, 2003
)
0.32
" Our objective was to analyze the effect of 2 surfactants with different affinity for P-gp in vitro on the intestinal absorption and bioavailability of the P-gp substrate talinolol in humans."( P-glycoprotein and surfactants: effect on intestinal talinolol absorption.
Alsenz, J; Bogman, K; Degen, L; Drewe, J; Gutmann, H; Hopfgartner, G; Zysset, Y, 2005
)
0.33
"This in vivo intraduodenal perfusion study showed that low concentrations of TPGS, close to the concentrations that showed P-gp inhibition in vitro, significantly increased the bioavailability of talinolol."( P-glycoprotein and surfactants: effect on intestinal talinolol absorption.
Alsenz, J; Bogman, K; Degen, L; Drewe, J; Gutmann, H; Hopfgartner, G; Zysset, Y, 2005
)
0.33
" The corresponding mean absolute oral bioavailability figures were 36, 32, 39, 42 and 32% for ampicillin and 76, 74, 85, 73 and 74% for antipyrine, respectively."( Excipient effects on gastrointestinal transit and drug absorption in beagle dogs.
Basit, AW; Coffin, MD; Parsons, GE; Peters, EE; Schulze, JD; Staton, JS; Vickers, AW, 2005
)
0.33
"Alpha-tocopheryl polyethylene glycol succinate (TPGS) has been used to enhance the bioavailability of poorly absorbed drugs and as a vehicle for drug delivery systems."( Enhanced anticancer efficacy of alpha-tocopheryl succinate by conjugation with polyethylene glycol.
Choi, MK; Chung, JH; Kim, SH; Lee, CH; Lee, E; Lee, YJ; Lim, SJ; Youk, HJ, 2005
)
0.33
" The oral bioavailability of paclitaxel in TPGS 400/ethanol (7."( Enhanced oral bioavailability of paclitaxel by D-alpha-tocopheryl polyethylene glycol 400 succinate in mice.
Chang, YW; Chao, YS; Chen, CT; Chiang, TH; Ho, PY; Lin, HL; Lo, YK; Wu, HY; Wu, SH; Yao, HT; Yeh, TK, 2008
)
0.35
" Subsequently, TPPG 1000 was tested for its ability to enhance the bioavailability of raloxifene - an established P-gp substrate -in fasted male rats."( Inhibiting efflux with novel non-ionic surfactants: Rational design based on vitamin E TPGS.
Buchanan, CM; Caflisch, GB; Edgar, KJ; Large, SE; Lightner, JW; Little, JL; Rice, PJ; Ruble, KM; Wacher, VJ; Wempe, MF; Wright, C, 2009
)
0.35
" Oral bioavailability of the 30/70 dispersion was, although lower compared to the marketed Sporanox formulation, significantly enhanced compared to the crystalline drug."( Itraconazole/TPGS/Aerosil200 solid dispersions: characterization, physical stability and in vivo performance.
Augustijns, P; Froyen, L; Houthoofd, K; Martens, JA; Mols, R; Van den Mooter, G; Van Eerdenbrugh, B; Van Humbeeck, J; Van Speybroeck, M, 2009
)
0.35
"Vitamin E tocopheryl polyethylene glycol succinate (TPGS) is known to enhance the bioavailability of poorly water-soluble drugs via solubility and permeability enhancement."( Tabletability assessment of conventional formulations containing Vitamin E tocopheryl polyethylene glycol succinate.
Jin, F; Tatavarti, A, 2010
)
0.36
" In vivo evaluation confirmed the advantages of the TPGS-emulsified PLGA NP formulation versus Taxol in promoting oral bioavailability of paclitaxel."( Enhanced oral bioavailability of paclitaxel formulated in vitamin E-TPGS emulsified nanoparticles of biodegradable polymers: in vitro and in vivo studies.
Feng, SS; Zhao, L, 2010
)
0.36
" Optimised FFB SMEDDS formulations were then selected for in-vivo bioavailability study."( Characterisation of fenofibrate dissolution delivered by a self-microemulsifying drug-delivery system.
Chen, CH; Chen, ET; Ho, HO; Ke, WT; Sheu, MT; Wei, JD, 2010
)
0.36
" Therefore, SDs obtained by MW technique using vitamin E TPGS as carrier provide a promising way to increase the dissolution rate and solubility of poorly bioavailable drugs."( Characterization of solid dispersions of itraconazole and vitamin E TPGS prepared by microwave technology.
De Zordi, N; Macchiavelli, S; Moneghini, M; Princivalle, F; Solinas, D, 2010
)
0.36
" In this study, the absolute bioavailability of BBR was studied, and the enhancing effects of D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) on intestinal absorption were investigated in rats."( Bioavailability study of berberine and the enhancing effects of TPGS on intestinal absorption in rats.
Chen, W; Fan, DJ; Lin, X; Meng, LK; Miao, YQ; Tang, X; Yang, SS, 2011
)
0.37
"SMEDDS, consisting of Myritol 318 and TPGS combined with Tween 80 at 4:1, was able to enhance the oral bioavailability of FFB."( In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate.
Chen, YC; Ho, HO; Ke, WT; Lin, YM; Sheu, MT; Su, YD; Wu, JY, 2011
)
0.37
" The clinical failure of the conventional oral therapy of griseofulvin is most likely attributed to its poor solubility and appreciable inter- and intra-subject variation in bioavailability from different commercial products."( Preparation and evaluation of dermal delivery system of griseofulvin containing vitamin E-TPGS as penetration enhancer.
Aggarwal, N; Goindi, S; Mehta, SD, 2012
)
0.38
" In an attempt to improve the bioavailability and the stability of four of these derivatives, we propose here two different approaches: complexation with β-cyclodextrin derivatives and incorporation of these substances inside antioxidant micelles."( Overcoming instability and low solubility of new cytostatic compounds: a comparison of two approaches.
Bauer-Brandl, A; di Cagno, M; Hlaváč, J; Skalko-Basnet, N; Stein, PC; Styskala, J, 2012
)
0.38
"To improve the solubility, permeability and oral bioavailability of cefpodoxime proxetil, β-lactam antibiotic."( Self-nanoemulsifying drug delivery system of cefpodoxime proxetil containing tocopherol polyethylene glycol succinate.
Bajaj, A; Khole, I; Munjapara, G; Rao, MR, 2013
)
0.39
"SNEDDS formulations led to improved oral bioavailability due to enhanced solubilization of selected drug."( Self-nanoemulsifying drug delivery system of cefpodoxime proxetil containing tocopherol polyethylene glycol succinate.
Bajaj, A; Khole, I; Munjapara, G; Rao, MR, 2013
)
0.39
" After administration of mangiferin at a dose of 30 mg/kg combining with sodium deoxycholate, the bioavailability of mangiferin increased four-fold, and this may be due to sodium deoxycholate weakening the compactness between lecithin molecules and increased the paracellular permeability."( Increased absorption of mangiferin in the gastrointestinal tract and its mechanism of action by absorption enhancers in rats.
Gu, Y; Meng, L; Ren, T; Tang, X; Tian, B; Wang, X; Zhang, Y, 2013
)
0.39
" Oral bioavailability of optimized LBOF (O-LBOF) was evaluated in male Sprague-Dawley (SD) rats at a dose of 250 mg/kg."( Novel lipid based oral formulation of curcumin: development and optimization by design of experiments approach.
Bansal, AK; Lale, SV; Munjal, B; Patel, SB; Pawar, YB; Purohit, H; Valicherla, GR, 2012
)
0.38
" The relative bioavailability of the micelles (AUC(0-∞)) compared with baohuoside I (AUC(0-∞)) was 533%, demonstrating great potential for clinical application."( A novel drug-phospholipid complex loaded micelle for baohuoside I enhanced oral absorption: in vivo and in vivo evaluations.
Jia, XB; Jin, X; Sun, E; Tan, XB; Zhang, ZH; Zhu, FX, 2013
)
0.39
" In addition, the experimental results from the formulation screening used in our study could be useful for enhancing the bioavailability of sirolimus in preformulation and formulation studies."( Supersaturatable formulations for the enhanced oral absorption of sirolimus.
Cha, KH; Cho, W; Hwang, SJ; Kim, JS; Kim, MS; Park, HJ; Park, J, 2013
)
0.39
" It can also act as a P-glycoprotein (P-gp) inhibitor and has been served as an excipient for overcoming multidrug resistance (MDR) and for increasing the oral bioavailability of many anticancer drugs."( The applications of Vitamin E TPGS in drug delivery.
Guo, Y; Luo, J; Otieno, BO; Tan, S; Zhang, Z, 2013
)
0.39
"A novel drug delivery system, TPGS 1000 (TPGS) emulsified zein nanoparticles (TZN), were designed with an objective to improve the oral bioavailability of daidzin, an isoflavone glycoside with estrogenic activities."( TPGS emulsified zein nanoparticles enhanced oral bioavailability of daidzin: in vitro characteristics and in vivo performance.
Gu, L; Zou, T, 2013
)
0.39
"The goal of this study was to demonstrate that MK-0364 solid dispersions can be developed as a means to increase the solubility and bioavailability of a poorly water-soluble drug, MK-0364."( Development of amorphous solid dispersion formulations of a poorly water-soluble drug, MK-0364.
McKelvey, C; Moser, J; Rege, B; Sotthivirat, S; Xu, W; Zhang, D, 2013
)
0.39
" Based on the area-under-the-curve (AUC), the bioavailability of DEX in the experimental group was significantly higher than that in the control group administrated with regular DEX."( Intravitreal administration of dexamethasone-loaded PLGA-TPGS nanoparticles for the treatment of posterior segment diseases.
Bu, S; Jiang, L; Xie, X; Yang, C; Zeng, Q; Zhang, L; Zheng, Y; Zhu, D, 2013
)
0.39
" The oral bioavailability studies were conducted in rats and the pharmacokinetic parameters were evaluated."( Preparation and evaluation in vitro and in vivo of docetaxel loaded mixed micelles for oral administration.
Dou, J; Liu, X; Zhai, G; Zhang, H; Zhang, M, 2014
)
0.4
"Mixed micelles were designed to increase oral bioavailability of Apigenin (Ap)."( Micelles of TPGS modified apigenin phospholipid complex for oral administration: preparation, in vitro and in vivo evaluation.
Abbad, S; Baraza, LD; Lv, H; Munyendo, WL; Waddad, AY; Zhang, Z; Zhou, J, 2013
)
0.39
" However Ber's low oral bioavailability restricts its wide application."( Solid dispersion of berberine-phospholipid complex/TPGS 1000/SiO₂: preparation, characterization and in vivo studies.
Chen, Y; Deng, J; Jia, X; Lv, H; Zhang, Z; Zhou, J, 2014
)
0.4
" Tween 80-emulsified SLNs showed enhanced intestinal absorption, lymphatic uptake, and relative oral bioavailability of docetaxel compared with Taxotere in rats."( Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake.
Cho, HJ; Kim, DD; Park, JW; Yoon, IS, 2014
)
0.4
"D-alpha-tocopheryl polyethylene glycol succinate (TPGS) is a vitamin E derivative that has been intensively applied as a vehicle for drug delivery systems to enhance drug solubility and increase the oral bioavailability of anti-cancer drugs."( D-alpha-tocopheryl polyethylene glycol succinate (TPGS) induces cell cycle arrest and apoptosis selectively in Survivin-overexpressing breast cancer cells.
Constantinou, AI; Constantinou, C; Neophytou, CM; Papageorgis, P, 2014
)
0.4
" However, it shows poor bioavailability when administered orally."( Effect of high-pressure homogenization on formulation of TPGS loaded nanoemulsion of rutin - pharmacodynamic and antioxidant studies.
Ali, J; Baboota, S; Sahni, JK; Sharma, S, 2015
)
0.42
"The present study was to formulate curcumin solid lipid nanoparticles (Cur-SLNs) with P-gp modulator excipients, TPGS and Brij78, to enhance the solubility and bioavailability of curcumin."( Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin.
Ji, H; Li, M; Ren, J; Tang, J; Wu, L; Zheng, N, 2016
)
0.43
" In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of Cur-SLNs on the bioavailability and intestinal absorption of curcumin."( Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin.
Ji, H; Li, M; Ren, J; Tang, J; Wu, L; Zheng, N, 2016
)
0.43
"27-folds greater than curcumin suspension and the relative bioavailability of Cur-SLNs was 942."( Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin.
Ji, H; Li, M; Ren, J; Tang, J; Wu, L; Zheng, N, 2016
)
0.43
"Cur-SLNs with TPGS and Brij78 could improve the oral bioavailability and intestinal absorption of curcumin effectively."( Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin.
Ji, H; Li, M; Ren, J; Tang, J; Wu, L; Zheng, N, 2016
)
0.43
"Enhanced oral bioavailability in nanoemulsions was achieved via the mechanism of the maintenance of drug solubilization in the gastrointestinal tract and the enhancement of lymphatic transport, which resulted in therapeutic improvement of cerebral ischemic reperfusion injury."( Enhanced oral absorption and therapeutic effect of acetylpuerarin based on D-α-tocopheryl polyethylene glycol 1000 succinate nanoemulsions.
Fang, Z; Lou, H; Ren, M; Sun, D; Wei, X; Xue, X; Zhang, X, 2014
)
0.4
"A growing number of poorly water-soluble drug have been discovered, but the poor bioavailability is a critical problem."( Physical and dissolution characterization of cilostazol solid dispersions prepared by hot melt granulation (HMG) and thermal adhesion granulation (TAG) methods.
Chen, YC; Chiou, JD; Ho, HO; Sheu, MT, 2014
)
0.4
"Poor drug penetration and rapid clearance after topical instillation of a drug formulation into the eyes are the major causes for the lower ocular bioavailability from conventional eye drops."( Dorzolamide-loaded PLGA/vitamin E TPGS nanoparticles for glaucoma therapy: Pharmacoscintigraphy study and evaluation of extended ocular hypotensive effect in rabbits.
Ahmad, FJ; Anwar, M; Garg, V; Jain, GK; Khar, RK; Talegaonkar, S; Warsi, MH, 2014
)
0.4
" The dissolution and oral bioavailability of lercanidipine was significantly increased by addition of surfactants."( Dissolution and bioavailability of lercanidipine-hydroxypropylmethyl cellulose nanoparticles with surfactant.
Baek, IH; Cho, W; Choo, GH; Ha, ES; Hwang, SJ; Jin, SE; Jung, YS; Kim, JS; Kim, MS, 2015
)
0.42
" To improve the anti-cancer effect and bioavailability of TAN, we developed a mixed micelle system constituted with D-α-tocopheryl polyethylene glycol succinate-graft-poly(D,L-lactide-co-glycolide) (TPGS-g-PLGA) copolymer and Pluronic F68."( TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy.
Chen, M; Fang, X; Li, Y; Wang, Y; Zhang, J; Zhou, D, 2014
)
0.4
" Resveratrol (Res) is a promising candidate for overcoming cancer chemoresistance, but it has low bioavailability due to poor absorption, and ready metabolism limits its application."( mPEG-b-PCL/TPGS mixed micelles for delivery of resveratrol in overcoming resistant breast cancer.
Chen, M; Chen, R; Morott, J; Repka, MA; Wang, S; Wang, Y, 2015
)
0.42
"The AMB-PLGA-TPGS NP system significantly improves the AMB bioavailability by improving its antifungal activities and reducing its toxicity, and thus, these NPs may become a good drug carrier for antifungal treatment."( Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo.
Cai, S; Hou, W; Liu, F; Sun, L; Tang, X; Zhang, R; Zhu, H, 2014
)
0.4
"This study aimed to design the chitosan coated TPGS liposome to enhance the bioavailability of Coenzyme Q10 (CoQ10)."( TPGS-chitosome as an effective oral delivery system for improving the bioavailability of Coenzyme Q10.
Han, HK; Shao, Y; Yang, L, 2015
)
0.42
" In conclusion, ITZ-loaded-TPP NPs significantly improved ITZ bioavailability by increasing its aqueous dispersibility and extending the duration of drug release, thereby improving the antifungal efficacy of the ITZ agent."( Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles.
Chen, H; Hu, B; Hu, Y; Li, S; Qiu, L; Wu, X; Zheng, Y, 2015
)
0.42
" This blended NP system can be achieved through a simple and effective nanoprecipitation technique, and possesses unique properties: i) improved long-term compatibility brought by PEG-based polymers; ii) reduced multidrug resistance mediated by P-glycoprotein (P-gp) in tumor cells and increased bioavailability of anticancer drugs by incorporation of TPGS; iii) the regulation of controlled release through polymer ratios and active targeting by FA."( Blended nanoparticle system based on miscible structurally similar polymers: a safe, simple, targeted, and surprisingly high efficiency vehicle for cancer therapy.
Huang, L; Liu, D; Liu, G; Liu, Y; Mei, L; Tao, W; Yu, Q; Zeng, X; Zhang, J; Zhu, X, 2015
)
0.42
"Soluplus(®) (SP) and D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS)-based solid dispersion (SD) formulations were developed by hot-melt extrusion (HME) to improve oral bioavailability of valsartan (VST)."( Soluplus®/TPGS-based solid dispersions prepared by hot-melt extrusion equipped with twin-screw systems for enhancing oral bioavailability of valsartan.
Cho, HJ; Kang, WS; Kim, DD; Lee, JY; Piao, J; Yoon, IS, 2015
)
0.42
"Vitamin E tocopherol polyethylene glycol succinate (TPGS) is a non-ionic surface active agent, known to enhance the bioavailability of lipophilic compounds via wettability, solubility, and in some cases permeability enhancement."( An Extrusion Spheronization Approach to Enable a High Drug Load Formulation of a Poorly Soluble Drug with a Low Melting Surfactant.
Kesisoglou, F; Tatavarti, A, 2015
)
0.42
" PEGylated γ-T3 also increased the oral bioavailability of γ-T3 by threefolds when compared to the bioavailability of γ-T3 formulated into a self-emulsified drug delivery system."( PEGylated γ-tocotrienol isomer of vitamin E: Synthesis, characterization, in vitro cytotoxicity, and oral bioavailability.
Abu-Fayyad, A; Alqahtani, S; Behery, F; Cardelli, JA; Carroll, JL; Ebrahim, H; El Sayed, KA; Kaddoumi, A; Nazzal, S; Sallam, AA; Sylvester, PW, 2015
)
0.42
" The dissolution and oral bioavailability of the nanoparticles were also evaluated in rats."( Development of megestrol acetate solid dispersion nanoparticles for enhanced oral delivery by using a supercritical antisolvent process.
Baek, IH; Ha, ES; Jung, Y; Kim, JS; Kim, MS; Moon, HR; Yoo, JW, 2015
)
0.42
" The Cmax and mean retention time (MRT0-24) for CUR-MPP-TPGS-MMs were both increased, and the relative bioavailability of micelle formulation to curcumin suspension was 927."( Evaluation in vitro and in vivo of curcumin-loaded mPEG-PLA/TPGS mixed micelles for oral administration.
Chu, L; Duan, Y; Liu, W; Tong, HH; Zhai, G; Zhang, B, 2016
)
0.43
"Poor bioavailability of Docetaxel (DCT) arising due to its low aqueous solubility and permeability limits its clinical utility."( Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity.
Datta, D; Dave, KM; Gayen, JR; Gupta, AP; Mitra, K; Riyazuddin, M; Singh, A; Syed, AA; Valicherla, GR, 2016
)
0.43
"D-Alpha-tocopheryl polyethylene glycol 1000 succinate (Tocofersolan, Vedrop), has been developed in Europe to provide an orally bioavailable source of vitamin E in children with cholestasis."( Oral Tocofersolan Corrects or Prevents Vitamin E Deficiency in Children With Chronic Cholestasis.
Baumann, U; de Micheaux, SL; Gottrand, F; Habes, D; Houwen, R; Jacquemin, E; Koot, B; Le Mouhaër, J; Monard, L; Nemeth, A; Scheenstra, R; Thébaut, A, 2016
)
0.43
" In-vivo CAR oral bioavailability from NMs dispersions and drug control solution was evaluated in Wistar rats."( Novel carvedilol paediatric nanomicelle formulation: in-vitro characterization and in-vivo evaluation.
Bernabeu, E; Bertera, FM; Buontempo, F; Cagel, M; Chiappetta, DA; Höcht, C; Moretton, MA; Parola, L; Taira, CA; Wegmann, M, 2017
)
0.46
" The improvement on drug oral bioavailability contributes to the potential of this NMs formulation to enhance CAR paediatric treatment."( Novel carvedilol paediatric nanomicelle formulation: in-vitro characterization and in-vivo evaluation.
Bernabeu, E; Bertera, FM; Buontempo, F; Cagel, M; Chiappetta, DA; Höcht, C; Moretton, MA; Parola, L; Taira, CA; Wegmann, M, 2017
)
0.46
"The aim of this study was to assess the effect of d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) on the physicochemical characterization and oral bioavailability of a novel l-sulpiride-loaded quaternary microcapsule (QMC)."( Development of a novel l-sulpiride-loaded quaternary microcapsule: Effect of TPGS as an absorption enhancer on physicochemical characterization and oral bioavailability.
Choi, HG; Choi, JS; Jin, SG; Kim, DS; Kim, DW; Kim, JO; Kim, KS; Oh, KT; Seo, YG; Yong, CS; Youn, YS, 2016
)
0.43
"Nanosuspension is one of the most promising strategies to improve the oral bioavailability of insoluble drugs."( A cost-effective method to prepare curcumin nanosuspensions with enhanced oral bioavailability.
Ding, Y; Li, L; Wang, C; Wang, Y; Zhao, J, 2017
)
0.46
"A novel oral drug delivery system, TPGS modified docetaxel proniosomes (DTX-TPGS-PNs), was designed to enhance the oral bioavailability and antitumor efficiency of the poorly water-soluble drug docetaxel."( Improved Bioavailability and Antitumor Effect of Docetaxel by TPGS Modified Proniosomes: In Vitro and In Vivo Evaluations.
Dang, Z; Du, J; Feng, J; Hu, K; Liu, H; Tu, L; Wang, L; Zhou, Y, 2017
)
0.46
"Recent work has developed solid drug nanoparticles (SDNs) of efavirenz that have been demonstrated, preclinically, improved oral bioavailability and the potential to enable up to a 50% dose reduction, and is currently being studied in a healthy volunteer clinical trial."( Assessment of interactions of efavirenz solid drug nanoparticles with human immunological and haematological systems.
Giardiello, M; Liptrott, NJ; McDonald, TO; Owen, A; Rannard, SP, 2018
)
0.48
"Liposomes can achieve a controlled release and an improved bioavailability of water- insoluble drug with minimized side effects."( Surface modification of paclitaxel-loaded liposomes using d-α-tocopheryl polyethylene glycol 1000 succinate: Enhanced cellular uptake and cytotoxicity in multidrug resistant breast cancer cells.
Baek, JS; Cho, CW; Han, SM; Hwang, SJ; Kim, MS, 2018
)
0.48
"0-folds augmentation in permeability and bioavailability of Mgf."( Improving the biopharmaceutical attributes of mangiferin using vitamin E-TPGS co-loaded self-assembled phosholipidic nano-mixed micellar systems.
Gaspar, BL; Katare, OP; Khurana, RK; Singh, B; Singh, KK; Welsby, G, 2018
)
0.48
" However, despite the therapeutic potential of NAR, its clinical development has been hindered due to low aqueous solubility and inefficient transport across biological membranes resulting in low bioavailability at tumor sites."( Augmented anticancer activity of naringenin-loaded TPGS polymeric nanosuspension for drug resistive MCF-7 human breast cancer cells.
Radhakrishnan, A; Rajamani, S; Sengodan, T; Thangavelu, S, 2018
)
0.48
"Herb borneol is usually used in clinics for the treatment of central nervous system illness, for its ability of blood-brain barrier permeability, although its poor water solubility and poor bioavailability limit its clinical application to some degree."( Conjugation of vitamin E-TPGS and guar gum to carry borneol for enhancing blood-brain barrier permeability.
Cen, Y; Cheng, K; Liu, Y; Rao, L; Zhang, H, 2018
)
0.48
" Although the oral bioavailability of suspensions of its solid forms is poor, addition of vitamin E D-alpha-tocopherol polyethylene glycol 1000 succinate to dosing vehicles improves the fraction absorbed of the compound in vivo."( Overcoming the Bile Salt-Mediated Formation of Nanocolloids That Inhibit Oral Absorption of VX-985.
Bransford, P; Dworakowski, W; Kumar, S; Medek, A; Mudunuri, P; Peresypkin, A; Randles, EG; Snyder, PW; Song, B, 2019
)
0.51
" The aim of the present study was to enhance the oral bioavailability and brain distribution of 6-Gingerol via polymeric micelles."( Preparation and
Adu-Frimpong, M; Kesse Firempong, C; Wang, Q; Wei, Q; Xu, X; Yu, J; Zhang, H; Zhen, L, 2020
)
0.56
" VNP suffers from low oral bioavailability owing to its low water solubility and extensive first-pass metabolism."( Optimized vinpocetine-loaded vitamin E D-α-tocopherol polyethylene glycol 1000 succinate-alpha lipoic acid micelles as a potential transdermal drug delivery system: in vitro and ex vivo studies.
Ahmed, OA; Ahmed, TA; Aljaeid, BM; Badr-Eldin, SM; El-Say, KM, 2019
)
0.51
"The aim of the present investigation was to fabricate and evaluate solid lipid nanoparticles (SLNs) of asenapine maleate (AM) to improve its oral bioavailability (BA)."( Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies.
Mundada, V; Patel, M; Sawant, K, 2019
)
0.51
"In this study, syringic acid-loaded TPGS liposome (SA-TPGS-Ls) was successfully prepared to improve oral bioavailability of syringic acid (SA)."( Preparation and Characterization of Syringic Acid-Loaded TPGS Liposome with Enhanced Oral Bioavailability and In Vivo Antioxidant Efficiency.
Adu-Frimpong, M; Li, W; Liu, Y; Sun, C; Wang, Q; Xu, X; Yu, J, 2019
)
0.51
"The present investigation highlights the development of D-α-Tocopheryl polyethylene glycol 1000 succinate (Tocophersolan; TPGS) stabilized lipid nanocapsules for enhancing the oral bioavailability and permeability of curcumin (CUR)."( Tocophersolan stabilized lipid nanocapsules with high drug loading to improve the permeability and oral bioavailability of curcumin.
Bapat, P; Chaudhari, D; Ghadi, R; Jain, S; Katiyar, SS, 2019
)
2.17
"Isoliquiritigenin (ISL) has a great variety of pharmacological effects especially liver cancer therapy, but its poor solubility, bioavailability and liver targeting have limited its clinical use."( Preparation, in vitro and in vivo evaluation of isoliquiritigenin-loaded TPGS modified proliposomes.
Adu-Frimpong, M; Ji, H; Liu, J; Toreniyazov, E; Wang, Q; Wei, C; Wei, Q; Weng, W; Xie, Y; Xu, X; Yu, J; Zhang, K, 2019
)
0.51
" Prolonged circulation half-life and tumor site bioavailability were achieved for both the drugs with the developed approach."( Targeted co-delivery of the aldose reductase inhibitor epalrestat and chemotherapeutic doxorubicin via a redox-sensitive prodrug approach promotes synergistic tumor suppression.
Banala, VT; Dwivedi, M; Gautam, S; Marwaha, D; Mishra, PR; Sharma, M; Sharma, S; Shukla, RP; Urandur, S, 2019
)
0.51
"This study was designed to investigate the bioavailability and targeting of myricetrin-loaded ternary micelles modified with and without TPGS."( The characterisation, pharmacokinetic and tissue distribution studies of TPGS modified myricetrin mixed micelles in rats.
Adu-Frimpong, M; Ji, H; Toreniyazov, E; Wang, Q; Wei, C; Wei, Q; Weng, W; Xie, Y; Xu, X; Yu, J, 2019
)
0.51
" However its drawbacks of low bioavailability and big individual difference remain to be improved in clinical application."( Rapamycin loaded TPGS-Lecithins-Zein nanoparticles based on core-shell structure for oral drug administration.
Lv, H; Xie, Z; Zhang, Z, 2019
)
0.51
"The results further highlights the potential of TPM as an additive in lipid formulations to improve the solubilization and oral bioavailability of poorly water-soluble compounds."( Differential Effects of TPM, A Phosphorylated Tocopherol Mixture, and Other Tocopherol Derivatives as Excipients for Enhancing the Solubilization of Co-Enzyme Q10 as a Lipophilic Drug During Digestion of Lipid- Based Formulations.
Boyd, BJ; Gavin, PD; Khan, JT; Libinaki, R; Pham, A; Ramirez, G, 2019
)
0.51
" These molecules help reduce gut pathogens, while enhancing the absorption and bioavailability of therapeutic drugs, phytomedicines, and nanomedicines."( Iron Transport Tocopheryl Polyethylene Glycol Succinate in Animal Health and Diseases.
DuBourdieu, D; Gupta, RC; Lall, R; Srivastava, A; Talukder, J, 2019
)
0.51
" The low bioavailability of raloxifene (2%) is the result of its low solubility and intestinal glucuronidation."( Vitamin E TPGS based transferosomes augmented TAT as a promising delivery system for improved transdermal delivery of raloxifene.
Ahmed, OAA; Alhakamy, NA; Fahmy, UA, 2019
)
0.51
" Nevertheless, low solubility and bioavailability hamper the application of SA."( Development of TPGS/F127/F68 mixed polymeric micelles: Enhanced oral bioavailability and hepatoprotection of syringic acid against carbon tetrachloride-induced hepatotoxicity.
Adu-Frimpong, M; Deng, W; Li, W; Li, Y; Ma, P; Sun, C; Xu, X; Yu, J; Zhang, H; Zhu, Y, 2020
)
0.56
"In this study, we developed ticagrelor-dispersed nanosuspension (TCG-NSP) to enhance the dissolution and oral bioavailability of ticagrelor (TCG) through a statistical design approach."( Development and evaluation of TPGS/PVA-based nanosuspension for enhancing dissolution and oral bioavailability of ticagrelor.
Baek, JS; Byeon, JJ; Cho, CW; Han, MG; Kim, MK; Lee, HK; Na, YG; Pham, TMA, 2020
)
0.56
" For these reasons, Tocophersolan has been widely used for improving the bioavailability of numerous pharmaceutical active ingredients."( Rediscovering Tocophersolan: A Renaissance for Nano-Based Drug Delivery and Nanotheranostic Applications.
Chen, S; Cui, Q; Wande, DP; Xiong, H; Xu, C; Yao, J, 2021
)
1.31
" Lopinavir is an HIV-1 protease inhibitor with low aqueous solubility leading to poor oral bioavailability and thus frequent dosing."( Central composite design-based optimization of lopinavir vitamin E-TPGS micelle: In vitro characterization and in vivo pharmacokinetic study.
Mahajan, HS; Patil, PH, 2020
)
0.56
"06-fold increase in relative bioavailability compared to that of the CUR suspension."( Enhanced oral bioavailability of self-assembling curcumin-vitamin E prodrug-nanoparticles by co-nanoprecipitation with vitamin E TPGS.
Adu-Frimpong, M; Chen, B; Deng, W; Sun, C; Xu, X; Yu, J; Zhang, H; Zhu, Y, 2020
)
0.56
" It improves the bioavailability of drugs through permeation enhancement and down-regulation of P-glycoproteins."( Nanocarriers based on vitamin E-TPGS: Design principle and molecular insights into improving the efficacy of anticancer drugs.
Bahadur, P; Rathod, S; Tiwari, S, 2021
)
0.62
"(1) Background: vitamin E is often supplemented in the form of tocopherol acetate, but it has poor bioavailability and can fail to correct blood tocopherol concentrations in some patients with severe cholestasis."( Comparison of α-Tocopherol, α-Tocopherol Acetate, and α-Tocopheryl Polyethylene Glycol Succinate 1000 Absorption by Caco-2 TC7 Intestinal Cells.
Blond, E; Bordat, C; Cuerq, C; Halimi, C; Nowicki, M; Peretti, N; Reboul, E, 2020
)
0.56
" Rat PK study demonstrated significantly higher etoposide bioavailability from TPGS vs."( Adequate formulation approach for oral chemotherapy: Etoposide solubility, permeability, and overall bioavailability from cosolvent- vs. vitamin E TPGS-based delivery systems.
Beig, A; Dahan, A; Fine-Shamir, N, 2021
)
0.62
" Although oral formulations are clinically available, the lower bioavailability (<2%) embarrasses the pharmaceutists."( Bioadhesive polymer/lipid hybrid nanoparticles as oral delivery system of raloxifene with enhancive intestinal retention and bioavailability.
Du, X; Gao, N; Song, X, 2021
)
0.62
"The oral bioavailability of curcumin is limited, attributed to its low solubility or dissolution and poor absorption."( Development of Gelucire
Amin, PD; Shinde, UK; Suryawanshi, DG, 2021
)
0.62
" However, being a P-glycoprotein efflux substrate with a limited oral bioavailability imposes a challenge to its clinical efficacy."( Hybrid lipid core chitosan-TPGS shell nanocomposites as a promising integrated nanoplatform for enhanced oral delivery of sulpiride in depressive disorder therapy.
Abdelmonsif, DA; Aly, RG; Elgindy, NA; Mohyeldin, SM; Ragab, D; Samy, WM, 2021
)
0.62
" In this study, TMC was used as a mucoadhesive adjuvant to enhance the oral bioavailability and hence antitumour effects of gemcitabine formulated into nanocomplexes composed of poly(lactic-co-glycolic acid) nanoparticles (PLGA NPs) conjugated with d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS)."( N-trimethyl chitosan coated nano-complexes enhance the oral bioavailability and chemotherapeutic effects of gemcitabine.
Chen, G; Li, H; Liu, M; Lu, W; Svirskis, D; Wen, J; Ying, M, 2021
)
0.62
"The oral bioavailability and efficacy of baicalein is dramatically limited by its low solubility and effect of efflux."( Application of TPGS as an efflux inhibitor and a plasticizer in baicalein solid dispersion.
Hua, D; Li, S; Tong, M; Wang, J; Wu, X; Yu, X; Zhang, S; Zhang, Z, 2022
)
0.72
"Nintedanib esylate is a kinase inhibitor designated for the cure of non-small cell lung cancer suffered from first-pass metabolism which resulted in low oral bioavailability (~ 4."( Bioavailability enhancement of vitamin E TPGS liposomes of nintedanib esylate: formulation optimization, cytotoxicity and pharmacokinetic studies.
Chinni, S; Kala, SG, 2022
)
0.72
" However, the absorption rate of berberine is less than 1% in humans."( Emulsification by vitamin E TPGS or Quillaja extract enhanced absorption of berberine without affecting its metabolism in humans.
Gu, L; Wang, GP; Yagiz, Y, 2022
)
0.72
" Furthermore, the in-vivo study showed that TPGS-NLC was able to enhance GEF bioavailability (1."( TPGS decorated NLC shift gefitinib from portal absorption into lymphatic delivery: Intracellular trafficking, biodistribution and bioavailability studies.
Alanazi, FK; Ali, EA; Alqahtani, AS; Attia, SM; Harisa, GI; Nasr, FA; Omran, GA; Sherif, AY, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
"01) plasma alpha-tocopherol concentrations during the three-week experimental period in sheep dosed with equivalent units of TA than in those dosed with TPGS."( Plasma alpha-tocopherol profiles in sheep after oral administration of dl-alpha-tocopheryl acetate and d-alpha-tocopheryl polyethylene glycol-1000 succinate.
Hidiroglou, M; Ivan, M, 1991
)
0.28
" The combination of PLGA/TPGS/PEG as safe pharmaceutical excipient to formulate particulate delivery system is beneficial in improving the pharmaceutical properties for further powder dosage application."( Novel powder formulations for controlled delivery of poorly soluble anticancer drug: application and investigation of TPGS and PEG in spray-dried particulate system.
Feng, SS; Mu, L; Ning, HZ; Tan, CS; Teo, MM, 2005
)
0.33
" Groups 3, 4 and 5 received four subcutaneous injections at six-hour intervals for total dosage of 800 IU/kg alpha-tocopherol, 1000 IU/kg gamma-tocopherol and 750 IU/kg TPGS, respectively."( Protective effects of vitamin E forms (alpha-tocopherol, gamma-tocopherol and d-alpha-tocopherol polyethylene glycol 1000 succinate) on retinal edema during ischemia-reperfusion injury in the guinea pig retina.
Aydemir, O; Celebi, S; Kükner, AS; Yekeler, H; Yilmaz, T,
)
0.13
" Vitamin E TPGS (VeTPGS), a non-ionic surfactant, has been used in both liquid and solid dosage forms to solubilize compounds and improve their bioavailability."( An investigation of the thermodynamic miscibility between VeTPGS and polymers.
Chiappetta, D; Li, J, 2008
)
0.35
" Animals dosed with raloxifene and TPPG 1000 experienced an increase in raloxifene oral bioavailability versus a control group which received no inhibitor."( Inhibiting efflux with novel non-ionic surfactants: Rational design based on vitamin E TPGS.
Buchanan, CM; Caflisch, GB; Edgar, KJ; Large, SE; Lightner, JW; Little, JL; Rice, PJ; Ruble, KM; Wacher, VJ; Wempe, MF; Wright, C, 2009
)
0.35
" Few studies have evaluated feasibility of formulating TPGS in conventional solid dosage forms such as tablets due to processing challenges resulting from its waxy nature and low melting point (approximately 37 degrees C)."( Tabletability assessment of conventional formulations containing Vitamin E tocopheryl polyethylene glycol succinate.
Jin, F; Tatavarti, A, 2010
)
0.36
"The objective of this study is to investigate processing challenges associated with the incorporation of Vitamin E TPGS (d-α tocopheryl polyethylene glycol 1000 succinate) into solid pharmaceutical dosage forms."( Processing challenges with solid dosage formulations containing vitamin E TPGS.
Bindra, DS; Gour, S; Hamey, R; Pandey, P; Sinko, PD; Vema-Varapu, C, 2013
)
0.39
" The potential solid dispersions would enable an oral solid dosage form as a monotherapy or combination product of MK-0364."( Development of amorphous solid dispersion formulations of a poorly water-soluble drug, MK-0364.
McKelvey, C; Moser, J; Rege, B; Sotthivirat, S; Xu, W; Zhang, D, 2013
)
0.39
"The paclitaxel nanosuspensions prepared in this study could markedly enhance the tolerance dosage in mice, and manifest different pharmacokinetic properties compared with the solution."( Paclitaxel nanosuspensions coated with P-gp inhibitory surfactants: I. Acute toxicity and pharmacokinetics studies.
Gao, L; Kang, J; Liu, G; Ma, J; Niu, M; Wang, H; Wang, X; Wang, Z, 2013
)
0.39
" Antileishmanial activity as revealed from selectivity index in wild-type strain was found to be significant for AGnp with TPGS in about one-tenth of the dosage of the free AG and one-third of the dosage of the AGnp without TPGS."( In vitro susceptibilities of wild and drug resistant leishmania donovani amastigote stages to andrographolide nanoparticle: role of vitamin E derivative TPGS for nanoparticle efficacy.
Bera, T; Das, S; Halder, A; Mondal, S; Mukherjee, A; Roy, P, 2013
)
0.39
" OPTN could be acted as a novel and new dosage form to be used in cancer treatment study."( A novel oleanolic acid-loaded PLGA-TPGS nanoparticle for liver cancer treatment.
Bao, X; Chu, QC; Gao, M; Guan, X; Jiang, N; Liu, KX; Tian, Y; Xu, H; Zhang, CH, 2015
)
0.42
" This was achieved by evaluating plasma, liver and adrenal gland concentrations of d-α-tocopheryl succinate (TS) and d-α-tocopherol as well as oxidative status of plasma following oral dosing of TPGS-containing vehicles, intraperitoneal (IP) dosing of TS or ex vivo treatment of blood with H2O2."( D-α-tocopheryl polyethylene glycol 1000 succinate-containing vehicles provide no detectable chemoprotection from oxidative damage.
Baumgart, BR; Bunch, RT; Davies, MH; Donegan, M; Lange, RW; Lentz, K; Salcedo, TW; Sanderson, TP; Simic, D; Van Vleet, TR, 2015
)
0.42
" We found that the surface modification of microparticles with HPMC and TPGS can be an effective formulation strategy for new dosage forms of poorly water-soluble active pharmaceutical ingredients (APIs) to provide higher solubility and dissolution."( Fabrication and evaluation of celecoxib microparticle surface modified by hydrophilic cellulose and surfactant.
Baek, IH; Cho, W; Choo, GH; Ha, ES; Hwang, SJ; Jeong, HY; Jung, YS; Kim, JS; Kim, MS; Noh, J; Ok, J, 2015
)
0.42
" Our results suggest that the use of a hybrid system may allow a decrease in the dosage regimen without the loss of therapeutic effect."( Novel nanosystem to enhance the antitumor activity of lapatinib in breast cancer treatment: Therapeutic efficacy evaluation.
Huo, ZJ; Liu, K; Liu, P; Pang, B; Wang, SJ; Wang, ZQ; Zuo, WS, 2015
)
0.42
" The use of vitamin E TPGS, however, in solid dosage forms is limited because of the processing challenges resulting from its waxy nature and low melting temperature (∼37°C)."( An Extrusion Spheronization Approach to Enable a High Drug Load Formulation of a Poorly Soluble Drug with a Low Melting Surfactant.
Kesisoglou, F; Tatavarti, A, 2015
)
0.42
" In the anticancer efficacy test with MCF-7/ADR tumor bearing nude mice, the DOX-loaded TPGS 2K micelles displayed significantly higher antitumor activity compared with free DOX solution at the same DOX dosage but less toxicity evaluated by the change of body weight and histological examination."( Micelles of d-α-Tocopheryl Polyethylene Glycol 2000 Succinate (TPGS 2K) for Doxorubicin Delivery with Reversal of Multidrug Resistance.
Chen, D; Hao, T; Li, Z; Liu, K; Liu, Y; Qi, Y; Sun, P; Tian, Y, 2015
)
0.42
" The liver-targeting RPTN, which displayed enhanced pharmacological effects and decreased toxicity for the loaded drug RBG, is therefore a promising intravenous dosage form that may be useful in the treatment of liver cancer."( Liver-targeting Resibufogenin-loaded poly(lactic-co-glycolic acid)-D-α-tocopheryl polyethylene glycol 1000 succinate nanoparticles for liver cancer therapy.
Chu, Q; Deng, S; Gao, M; Guan, X; Huo, X; Liu, H; Liu, K; Ma, X; Tian, Y; Xu, H, 2016
)
0.43
" In this study, TPGS induced apoptotic cell death in Jurkat cells, but not in PBL, in a dose-response manner with increasing nuclear DNA fragmentation, increasing cell cycle arrest, and decreasing ΔΨm."( Vitamin E synthetic derivate-TPGS-selectively induces apoptosis in jurkat t cells via oxidative stress signaling pathways: implications for acute lymphoblastic leukemia.
Jimenez-Del-Rio, M; Lopez-Osorio, B; Ruiz-Moreno, C; Sierra-Garcia, L; Velez-Pardo, C, 2016
)
0.43
" Its tissue distribution in rats may change with different dosage forms, which therefore shall be studied after ARS-TPGS-Lipo was injected."( [Tissue distribution of TPGS modified artesunate liposome and its metabolites in rats].
An, R; Hu, C; Liang, K; Wang, XH; You, LS, 2018
)
0.48
" Although the oral bioavailability of suspensions of its solid forms is poor, addition of vitamin E D-alpha-tocopherol polyethylene glycol 1000 succinate to dosing vehicles improves the fraction absorbed of the compound in vivo."( Overcoming the Bile Salt-Mediated Formation of Nanocolloids That Inhibit Oral Absorption of VX-985.
Bransford, P; Dworakowski, W; Kumar, S; Medek, A; Mudunuri, P; Peresypkin, A; Randles, EG; Snyder, PW; Song, B, 2019
)
0.51
"Overall, the nano-complex may serve as a promising local therapeutic patch against MDR CRC with one-time dosing to achieve a long-term tumor control."( A personalized and long-acting local therapeutic platform combining photothermal therapy and chemotherapy for the treatment of multidrug-resistant colon tumor.
Chen, Y; Chen, ZS; Gao, W; Jiang, Y; Lin, Z; Wang, B; Wu, S; Yang, X, 2018
)
0.48
" The in vivo anesthesia antinociception study displayed that NLCs showed stronger and longer anesthesia antinociceptive effect when compared with single drugs loaded NLCs and drugs solution even at a lower dosage of drugs."( Topical anesthetic analgesic therapy using the combination of ropivacaine and dexmedetomidine: hyaluronic acid modified long-acting nanostructured lipid carriers containing a skin penetration enhancer.
Chao, L; Liu, Y; Qiu, D; Yang, Y, 2019
)
0.51
" Due to its extremely low solubility in water, it was difficult to develop an injectable liquid dosage form."( Injected laquinimod D-α-tocopheryl polyethylene glycol-1000 succinate polymeric micelles for the treatment of inflammatory bowel disease.
Chen, R; Tong, M; Wang, L; Xu, H; Xue, P; Yang, W; Yao, Q; Yuan, J; Zhao, Y; ZhuGe, D, 2020
)
0.56
" RLX fails to be developed into injectable dosage forms due to poor solubility."( Bioadhesive polymer/lipid hybrid nanoparticles as oral delivery system of raloxifene with enhancive intestinal retention and bioavailability.
Du, X; Gao, N; Song, X, 2021
)
0.62
"Delivering therapeutics to the brain using conventional dosage forms is always a challenge, thus the present study was aimed to formulate mucoadhesive nanoemulsion (MNE) of aripiprazole (ARP) for intranasal delivery to transport the drug directly to the brain."( Antipsychotic Potential and Safety Profile of TPGS-Based Mucoadhesive Aripiprazole Nanoemulsion: Development and Optimization for Nose-To-Brain Delivery.
Choudhury, H; Gorain, B; Kokare, CR; Kumbhar, SA; Shrivastava, B, 2021
)
0.62
"Based on the optimization of particle size and embedding rate of PTX-loaded mixed NPs, the appropriate dosage ratio of FA-F87-PLGA to TPGS was finally determined to be 5:3."( Preparation and In Vitro/Vivo Evaluation of Folate-conjugated Pluronic F87-PLGA/TPGS Mixed Nanoparticles for Targeted Drug Delivery.
Gong, Y; Li, Y; Li, Z; Wu, T; Xiong, X, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Occurs in Manufacturing (1 Product(s))

Product Categories

Product CategoryProducts
Vitamins & Supplements1

Products

ProductBrandCategoryCompounds Matched from IngredientsDate Retrieved
NutriBiotic Nasal Spray Plus -- 1 fl ozNutriBioticVitamins & Supplementsascorbic acid, goldenseal, glycerin, tocophersolan, xylitol2024-11-29 10:47:42

Drug Classes (1)

ClassDescription
tocolA chromanol with a chroman-6-ol skeleton that is substituted at position 2 by a saturated or triply-unsaturated hydrocarbon chain consisting of three isoprenoid units.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (565)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (0.88)18.7374
1990's15 (2.65)18.2507
2000's60 (10.62)29.6817
2010's376 (66.55)24.3611
2020's109 (19.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.74

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.74 (24.57)
Research Supply Index6.38 (2.92)
Research Growth Index5.66 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index3.00 (0.95)

This Compound (20.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (1.73%)5.53%
Reviews15 (2.60%)6.00%
Case Studies3 (0.52%)4.05%
Observational1 (0.17%)0.25%
Other549 (94.98%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]