Page last updated: 2024-12-06

cremophor el

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Description

cremophor EL: solvent for Althesin & Propanidid implicated as possible cause of similar adverse effects polyethoxylated castor oil; RN given refers to cpd with unknown MF; see also records for cremophor & cremophor A [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID104840
SCHEMBL ID830352
MeSH IDM0040672

Synonyms (4)

Synonym
cremophor el
63393-92-0
SCHEMBL830352
oxirane;propane-1,2,3-triol

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Paclitaxel elastic liposomal formulation seems to be a better alternative for safe and effective delivery of paclitaxel."( Evaluation of biosafety and intracellular uptake of Cremophor EL free paclitaxel elastic liposomal formulation.
Jain, S; Tiwary, AK; Utreja, P, 2012
)
0.38
" Studies indicate that Cremophors, especially EL, have toxic side effects, but few data are available on endothelial and epithelial cells, which form biological barriers and are directly exposed to these molecules."( Kinetic analysis of the toxicity of pharmaceutical excipients Cremophor EL and RH40 on endothelial and epithelial cells.
Bocsik, A; Deli, MA; Kiss, L; Ozsvári, B; Puskás, LG; Szabó-Révész, P; Veszelka, S; Walter, FR, 2013
)
0.39
"The toxic effects of paclitaxel (PTX) and its solubilizing agent cremophor EL (CREL) have been well established in vitro; however, the in vivo mechanisms underlying this toxicity remain unclear."( Systemic toxicity induced by paclitaxel in vivo is associated with the solvent cremophor EL through oxidative stress-driven mechanisms.
Campos, FC; Cecchini, AL; Cecchini, R; Martins-Pinge, MC; Panis, C; Victorino, VJ, 2014
)
0.4
" The stability study indicated that the system was stable for storage and dilution with distilled water, while the safety testing showed that the micelle was safe for intravenous administration with low hemolysis rates and low allergic reaction rates."( A Novel Dantrolene Sodium-Loaded Mixed Micelle Containing a Small Amount of Cremophor EL: Characterization, Stability, Safety and Pharmacokinetics.
Jiang, D; Jin, W; Li, H; Meng, Y; Song, H; Tan, X; Wen, J; Zhang, Y; Zheng, W, 2019
)
0.51

Pharmacokinetics

The aim of the present study was to determine whether Cremophor EL is a suitable surfactant that can be routinely applied to pharmacokinetic (PK) studies in early drug discovery. The population model was able to adequately describe the pharmacokeretic parameters and influence of covariates on the pharmacokinet.

ExcerptReferenceRelevance
"Studies in humans and mice have demonstrated a nonlinear pharmacokinetic behavior of paclitaxel."( Nonlinear pharmacokinetics of paclitaxel in mice results from the pharmaceutical vehicle Cremophor EL.
Beijnen, JH; Nooijen, WJ; Sparreboom, A; van Tellingen, O, 1996
)
0.29
" Pharmacokinetic sampling was performed during the first and the second course, and the samples were analyzed using a validated high-performance liquid chromatographic assay."( Cremophor EL pharmacokinetics in a phase I study of paclitaxel (Taxol) and carboplatin in non-small cell lung cancer patients.
Beijnen, JH; Boschma, MU; Giaccone, G; Huizing, MT; Meerum Terwogt, J; Nannan Panday, VR; Schellens, JH; ten Bokkel Huinink, WW; van Tellingen, O; Veenhof, CH, 2000
)
0.31
" Based on these findings, we prospectively re-evaluated the linearity of paclitaxel disposition in patients using whole blood and plasma analysis, and sought to define a new pharmacokinetic model to describe the data."( Pharmacokinetic modeling of paclitaxel encapsulation in Cremophor EL micelles.
Brouwer, E; de Bruijn, P; Karlsson, MO; Nooter, K; Sparreboom, A; Stoter, G; van Zuylen, L; Verweij, J, 2001
)
0.31
" Pharmacokinetic parameters of unbound and total cisplatin and of topotecan lactone and total drug were not significantly different from historic control values (P>or=0."( Modulation of cisplatin pharmacodynamics by Cremophor EL: experimental and clinical studies.
Brouwer, E; de Jonge, MJ; Gelderblom, H; Loos, WJ; Nooter, K; Sparreboom, A; Stoter, G; van der Burg, ME; Verweij, J, 2002
)
0.31
"1 of paclitaxel suggests that the drugs might also interact at the pharmacodynamic level."( Pharmacokinetics and pharmacodynamics of combination chemotherapy with paclitaxel and epirubicin in breast cancer patients.
Baldini, E; Bocci, G; Conte, PF; Danesi, R; Del Tacca, M; Di Paolo, A; Fogli, S; Gennari, A; Innocenti, F; Salvadori, B, 2002
)
0.31
"The purpose of this study was to develop a population pharmacokinetic model for Cremophor EL used as a formulation vehicle for paclitaxel."( A population analysis of the pharmacokinetics of Cremophor EL using nonlinear mixed-effect modelling.
Beijnen, JH; Mathôt, RA; Schellens, JH; van den Bongard, HJ; van Tellingen, O, 2002
)
0.31
" The nonlinear mixed-effect modelling (NONMEM) program was used for the population pharmacokinetic analysis."( A population analysis of the pharmacokinetics of Cremophor EL using nonlinear mixed-effect modelling.
Beijnen, JH; Mathôt, RA; Schellens, JH; van den Bongard, HJ; van Tellingen, O, 2002
)
0.31
" The following pharmacokinetic parameters were estimated: volume of the central compartment (V1=2."( A population analysis of the pharmacokinetics of Cremophor EL using nonlinear mixed-effect modelling.
Beijnen, JH; Mathôt, RA; Schellens, JH; van den Bongard, HJ; van Tellingen, O, 2002
)
0.31
"The population model was able to adequately describe the pharmacokinetic parameters and influence of covariates on the pharmacokinetics of Cremophor EL."( A population analysis of the pharmacokinetics of Cremophor EL using nonlinear mixed-effect modelling.
Beijnen, JH; Mathôt, RA; Schellens, JH; van den Bongard, HJ; van Tellingen, O, 2002
)
0.31
" The hypersensitivity evaluation and pharmacokinetic behavior in rats were conducted to assess the new microemulsion."( An alternative paclitaxel microemulsion formulation: hypersensitivity evaluation and pharmacokinetic profile.
He, L; Wang, GL; Zhang, Q, 2003
)
0.32
" The goal of this study was to develop a semimechanistic population pharmacokinetic model to study the influence of CrEL on the oral absorption of paclitaxel."( Population pharmacokinetics of orally administered paclitaxel formulated in Cremophor EL.
Beijnen, JH; de Jonge, ME; Huitema, AD; Rodenhuis, S; Schellens, JH, 2005
)
0.33
" A population pharmacokinetic model was developed using the nonlinear mixed effect modelling program NONMEM."( Population pharmacokinetics of orally administered paclitaxel formulated in Cremophor EL.
Beijnen, JH; de Jonge, ME; Huitema, AD; Rodenhuis, S; Schellens, JH, 2005
)
0.33
" Covariate analysis did not reveal significant relationships with any of the pharmacokinetic parameters."( Population pharmacokinetics of orally administered paclitaxel formulated in Cremophor EL.
Beijnen, JH; de Jonge, ME; Huitema, AD; Rodenhuis, S; Schellens, JH, 2005
)
0.33
"A pharmacokinetic model was developed that described the pharmacokinetics of orally administered paclitaxel."( Population pharmacokinetics of orally administered paclitaxel formulated in Cremophor EL.
Beijnen, JH; de Jonge, ME; Huitema, AD; Rodenhuis, S; Schellens, JH, 2005
)
0.33
"The aim of this study was to increase the understanding on the pharmacokinetic and tissue distribution of paclitaxel as influenced by formulation approach."( In vivo pharmacokinetic and tissue distribution studies in mice of alternative formulations for local and systemic delivery of Paclitaxel: gel, film, prodrug, liposomes and micelles.
Dhanikula, AB; Panchagnula, R; Singh, DR, 2005
)
0.33
" The purpose was to compare the two pharmacokinetic model structures when only total paclitaxel concentrations are available."( Comparison of two types of population pharmacokinetic model structures of paclitaxel.
Fransson, M; Gréen, H, 2008
)
0.35
" The pharmacokinetic behavior may depend on the interval between the intravenous administration of the two drugs."( Paclitaxel and pegylated liposomal doxorubicin in recurrent head and neck cancer: clinical and unexpected pharmacokinetic interactions.
Airoldi, M; Cattel, L; Dosio, F; Garzaro, M; Milla, P; Pedani, F,
)
0.13
" Co-administration of PLD markedly reduced Cmax and the area under the curve (AUC), and increased PTX clearance."( Paclitaxel and pegylated liposomal doxorubicin in recurrent head and neck cancer: clinical and unexpected pharmacokinetic interactions.
Airoldi, M; Cattel, L; Dosio, F; Garzaro, M; Milla, P; Pedani, F,
)
0.13
" The PTX pharmacokinetic profile was unexpectedly affected by different administration time intervals; in the 0 h arm the AUC was reduced to one fourth, therefore a schedule with PTX on day one, PLD on day two may be preferred."( Paclitaxel and pegylated liposomal doxorubicin in recurrent head and neck cancer: clinical and unexpected pharmacokinetic interactions.
Airoldi, M; Cattel, L; Dosio, F; Garzaro, M; Milla, P; Pedani, F,
)
0.13
" Body weight change and neutropenia were assessed as pharmacodynamic markers of toxicity."( Differential pharmacodynamic effects of paclitaxel formulations in an intracranial rat brain tumor model.
Harrold, JM; Mager, DE; Mazurchuk, RV; Straubinger, RM; Tamburlin, JH; Zhou, R, 2010
)
0.36
" Plasma pharmacokinetic parameters of valspodar in its polymeric micellar formulation were compared to its clinical formulation, which uses Cremophor EL and ethanol as solubilizing agents."( Development of a polymeric micellar formulation for valspodar and assessment of its pharmacokinetics in rat.
Binkhathlan, Z; Brocks, DR; Hamdy, DA; Lavasanifar, A, 2010
)
0.36
" For the 340 mg/m(2) treatment arm, AUC(INF) was similar between both formulations; Cmax was 17% lower for the suspension versus the injection formulation."( Tanespimycin pharmacokinetics: a randomized dose-escalation crossover phase 1 study of two formulations.
Berman, D; Burris, HA; Jones, S; Murthy, B, 2011
)
0.37
" In this study we used the population pharmacokinetic approach to explore the influence of predicted Cremophor EL concentrations on paclitaxel (Taxol) metabolites."( Influence of Cremophor EL and genetic polymorphisms on the pharmacokinetics of paclitaxel and its metabolites using a mechanism-based model.
Fransson, MN; Friberg, LE; Gréen, H; Litton, JE, 2011
)
0.37
" The results of pharmacokinetic and distribution properties of PTX in the microemulsion were similar to those of the PTX injection."( A novel paclitaxel microemulsion containing a reduced amount of Cremophor EL: pharmacokinetics, biodistribution, and in vivo antitumor efficacy and safety.
Chen, S; Nie, SF; Pan, WS; Wang, X; Wang, Y; Wu, KC; Zhang, Q; Zhang, X; Zhao, BX; Zhao, X, 2011
)
0.37
"The two formulations presented different pharmacokinetic behaviour."( Pharmacokinetics, tissue distribution and anti-tumour efficacy of paclitaxel delivered by polyvinylpyrrolidone solid dispersion.
Chen, X; Liu, X; Scott, H; Sun, J; Wang, S; Zhang, Q; Zhang, X, 2012
)
0.38
" In the present study, intracellular uptake, repeated dose 28 days sub-acute toxicity, anti-cancer activity, biodistribution and pharmacokinetic studies were conducted to determine in vivo performance of CF-PTX formulation in comparison to marketed paclitaxel formulation."( Anti-cancer, pharmacokinetic and biodistribution studies of cremophor el free alternative paclitaxel formulation.
Jain, SK; Kumar, N; Mahajan, M; Roy, P; Tiwary, AK; Utreja, P, 2014
)
0.4
" In vivo anti-cancer activity of CF-PTX was evaluated using Ehrlich ascites carcinoma (EAC) model in mice followed by biodistribution and pharmacokinetic studies."( Anti-cancer, pharmacokinetic and biodistribution studies of cremophor el free alternative paclitaxel formulation.
Jain, SK; Kumar, N; Mahajan, M; Roy, P; Tiwary, AK; Utreja, P, 2014
)
0.4
" Pharmacokinetic and biodistribution studies showed sustained plasma concentration of paclitaxel depicted by higher mean residence time (MRT; 18."( Anti-cancer, pharmacokinetic and biodistribution studies of cremophor el free alternative paclitaxel formulation.
Jain, SK; Kumar, N; Mahajan, M; Roy, P; Tiwary, AK; Utreja, P, 2014
)
0.4
"The aim of the present study was to determine whether Cremophor EL is a suitable surfactant that can be routinely applied to pharmacokinetic (PK) studies in early drug discovery without influencing the intrinsic PK characteristics of the new chemical entities (NCEs)."( Use of solubilizers in preclinical formulations: Effect of Cremophor EL on the pharmacokinetic properties on early discovery compounds.
Gordon, WP; Groessl, T; Liu, B; Richmond, W; Tuntland, T, 2016
)
0.43
" Pharmacokinetic evaluations confirmed the longer retention of PTX in systemic circulation."( Formulation, optimization, hemocompatibility and pharmacokinetic evaluation of PLGA nanoparticles containing paclitaxel.
Ajmal, G; Bonde, GV; Kapoor, R; Mishra, B; Mittal, A; Mittal, P; Vardhan, H, 2019
)
0.51
" Pharmacokinetic (PK) studies were conducted in mice and the SBE-β-CD based formulation was compared with the Cremophor EL formulation."( Pharmacokinetic modeling of the blood-stable camptothecin analog AR-67 in two different formulations.
Adane, E; Leggas, M; Liu, X; Tang, F, 2019
)
0.51

Bioavailability

Cremophor EL is an 'inactive' pharmaceutic aid known to inhibit PGP in vitro. Results suggest that surfactants such as Cremophar EL and Polysorbate 80 should not only support solubilization but can also modulate the P-glycoprotein system.

ExcerptReferenceRelevance
" Diazepam, which produces good tranquilization, is well absorbed when given orally though absorption is influenced by other drugs given at the same time."( New drugs--boon or bane? Premedication and intravenous induction agents.
Clarke, RS, 1983
)
0.27
" The solubility, metabolism, bioavailability and effectiveness of O6-benzylguanine as an adjuvant therapy with BCNU were compared using two vehicles, cremophor-EL and PEG 400."( Biodistribution of O6-benzylguanine and its effectiveness against human brain tumor xenografts when given in polyethylene glycol or cremophor-EL.
Dolan, ME; Flora, KP; Friedman, HS; Grever, MR; Moschel, RC; Pegg, AE; Vishnuvajjala, BR, 1994
)
0.29
") instillation of saline suspended CyA to adult rats, the CyA plasma levels peaked at 30 min with a bioavailability of 78."( Pulmonary delivery of intratracheally instilled and aerosolized cyclosporine A to young and adult rats.
Dahlback, M; Eirefelt, S; Karlsson, BW; Lundin, PD; Pierzynowski, SG; Podlesny, J; Siwinska-Golebiowska, H; Taljanski, W; Westrom, BR, 1997
)
0.3
" These results suggest that surfactants such as Cremophor EL and Polysorbate 80 should not only support solubilization but can also modulate the P-glycoprotein system to improve the bioavailability of poorly absorbed drugs."( Effect of polyoxyl 35 castor oil and Polysorbate 80 on the intestinal absorption of digoxin in vitro.
Cloarec, A; Cornaire, G; Decourt, S; Houin, G; Legendre, JY; Saivin, S; Woodley, JF, 2000
)
0.31
"Recent studies in mice and patients have shown that the low oral bioavailability of paclitaxel can be increased by coadministration of P-glycoprotein blockers."( Entrapment by Cremophor EL decreases the absorption of paclitaxel from the gut.
Bardelmeijer, HA; Beijnen, JH; Malingré, MM; Ouwehand, M; Schellens, J; van Tellingen, O, 2002
)
0.31
" The bioavailability of paclitaxel was 31."( Influence of Cremophor El on the bioavailability of intraperitoneal paclitaxel.
Buijs, D; Gelderblom, H; Nooter, K; Ouwens, L; Sparreboom, A; Stoter, G; van Zomeren, DM; Verweij, J, 2002
)
0.31
" It was the aim of this study to test whether the extremely low bioavailability of saquinavir can be increased dose-dependently in vivo by cremophor EL, an 'inactive' pharmaceutic aid known to inhibit PGP in vitro."( Dose-dependent increase of saquinavir bioavailability by the pharmaceutic aid cremophor EL.
Burhenne, J; Ding, R; Fricker, R; Haefeli, WE; Martin-Facklam, M; Mikus, G; Walter-Sack, I, 2002
)
0.31
" However, oral bioavailability of this highly lipophilic compound is extremely poor (<1%)."( Enhanced transport of a novel anti-HIV agent--cosalane and its congeners across human intestinal epithelial (Caco-2) cell monolayers.
Cushman, M; Hejchman, E; Mitra, AK; Pal, D; Patel, J; Udata, C, 2003
)
0.32
" The apparent first-order absorption rate constant from the peritoneal cavity (k(a)) of TXL was about one-twentieth of that of TXT."( Disposition kinetics of taxanes after intraperitoneal administration in rats and influence of surfactant vehicles.
Furui, N; Furukawa, H; Fushida, S; Ishizaki, J; Jin, M; Miwa, K; Miyamoto, K; Nomura, M; Yamazaki, M; Yokogawa, K; Yoshihara, H, 2004
)
0.32
" The formulation was tested to determine its bioavailability enhancement in a non-flush/non-ligated rat ileal model."( Enhanced ileal absorption of a hydrophilic macromolecule, pentosan polysulfate sodium (PPS).
Dong, L; Nguyen, J; Wong, P; Yum, A, 2004
)
0.32
"The present study revealed that the self-nanoemulsified drug delivery system of all-trans-retinol acetate increased its dissolution rate and has the potential to enhance its bioavailability without interaction or incompatibility between the ingredients."( Preparation and in vitro characterization of self-nanoemulsified drug delivery system (SNEDDS) of all-trans-retinol acetate.
Al-Saidan, S; Khan, MA; Samy, AM; Taha, EI, 2004
)
0.32
" The bioavailability of paclitaxel was independent of the dose and of CrEL."( Population pharmacokinetics of orally administered paclitaxel formulated in Cremophor EL.
Beijnen, JH; de Jonge, ME; Huitema, AD; Rodenhuis, S; Schellens, JH, 2005
)
0.33
" Oral bioavailability was studied on prepared SMEDDS hard capsules and compared with that of the conventional tablet in Beagle dogs in vivo."( [Preparation and evaluation of self-microemulsifying drug delivery systems containing atorvastatin].
Li, ZD; Shen, HR; Zhong, MK, 2005
)
0.33
" Oral bioavailability of atorvastatin SMEDDS was greater than that of the conventional tablet."( [Preparation and evaluation of self-microemulsifying drug delivery systems containing atorvastatin].
Li, ZD; Shen, HR; Zhong, MK, 2005
)
0.33
"To investigate the impact of a change in the proportions of lipid, surfactant and co-solvent on the solubilisation capacity of self-emulsifying formulations of danazol during in vitro dispersion and digestion studies and correlation with in vivo bioavailability in beagle dogs."( Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs.
Charman, WN; Cuiné, JF; Edwards, GA; Porter, CJ; Pouton, CW, 2007
)
0.34
" The relative bioavailability of danazol after administration of a series of these formulations was also determined."( Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs.
Charman, WN; Cuiné, JF; Edwards, GA; Porter, CJ; Pouton, CW, 2007
)
0.34
" Consistent with these data, the bioavailability of danazol decreased significantly when the lipid content in the formulations was reduced."( Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs.
Charman, WN; Cuiné, JF; Edwards, GA; Porter, CJ; Pouton, CW, 2007
)
0.34
"Self-microemulsifying drug delivery systems (SMEDDS) are useful to improve the bioavailability of poorly water-soluble drugs by increasing their apparent solubility through solubilization."( Application of mixture experimental design to simvastatin apparent solubility predictions in the microemulsifion formed by self-microemulsifying.
Meng, J; Zheng, L, 2007
)
0.34
" 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
"Self-microemulsifying drug delivery systems (SMEDDS) were developed to overcome the problems of delivery and administration of piroxicam, a drug with low bioavailability and gastrointestinal irritation, The in vitro properties of it were assessed."( [Design and in vitro evaluation of self-microemulsifying drug delivery systems for piroxicam].
Nie, SF; Pan, WS; Sun, JY; Wang, J; Wang, Y; Zhou, XT, 2008
)
0.35
"This study aims to formulate and evaluate bioavailability of a self-nanoemulsified drug delivery system (SNEDDS) of a poorly water-soluble herbal active component oleanolic acid (OA) for oral delivery."( Formulation development and bioavailability evaluation of a self-nanoemulsified drug delivery system of oleanolic acid.
Chan, CK; Chang, Q; Meng, ZY; Sun, JB; Tong, HH; Wang, GN; Wang, YT; Xi, J; Zheng, Y, 2009
)
0.35
"P-glycoprotein (P-gp) located in the apicalmembranes of intestinal absorptive cells is an energy-dependent efflux pump which can reduce the bioavailability of a wide range of substrate drugs."( [Advances in the study of excipient inhibitors of intestinal P-glycoprotein].
Huang, JG; Li, G; Si, LQ; Yan, F, 2008
)
0.35
" The first-order peritoneal cavity-systemic circulation absorption rate constant of paclitaxel was 1/8 that of docetaxel."( Surfactants influence the distribution of taxanes in peritoneal dissemination tumor-bearing rats.
Ito, C; Kamijo, Y; Miyamoto, K; Nomura, M; Sai, Y, 2010
)
0.36
"A microemulsion system of docetaxel was prepared and evaluated for its solubilization capacity and oral bioavailability improvement."( Docetaxel microemulsion for enhanced oral bioavailability: preparation and in vitro and in vivo evaluation.
Choi, MK; Chung, SJ; Cui, FD; Kim, DD; Kim, JS; Mu, CF; Shim, CK; Yin, YM, 2009
)
0.35
" The mean bioavailability of valspodar was 42."( Pharmacokinetics of PSC 833 (valspodar) in its Cremophor EL formulation in rat.
Binkhathlan, Z; Brocks, DR; Hamdy, DA; Lavasanifar, A, 2010
)
0.36
"38 mg/kg had the larger AUC(0-t), the longer half-life and the prolonged circulation time with the mean bioavailability of 80."( Preparation of lorazepam-loaded microemulsions for intranasal delivery and its pharmacokinetics.
Hou, L; Sun, L; Yao, J; Zhang, ZQ; Zhou, JP, 2009
)
0.35
"To enhance oral bioavailability of matrine, a dedicated and newly emerging drug system called self-nanoemulsifying drug delivery system (SNEDDSs) was developed."( Preparation and evaluation of self-nanoemulsified drug delivery systems (SNEDDSs) of matrine based on drug-phospholipid complex technique.
Gong, T; Hao, X; Liu, J; Ruan, J; Yang, F; Zhang, Z; Zhu, D, 2010
)
0.36
"The objective of the present study was to formulate a microemulsion system for oral administration to improve the solubility and bioavailability of fenofibrate."( Design of fenofibrate microemulsion for improved bioavailability.
Hu, L; Jia, Y; Niu, F; Wu, H; Yan, C; Yang, X, 2011
)
0.37
"Carvedilol, a widely prescribed cardiovascular drug for hypertension and congestive heart failure, exhibits low and variable bioavailability owing to poor absorption and extensive hepatic first-pass metabolism."( Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential.
Bandyopadhyay, S; Kapil, R; Katare, OO; Khurana, L; Singh, B, 2011
)
0.37
" By virtue of extensive presystemic clearance, RLX bioavailability is only 2%."( Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal.
Abdallah, OY; Elnaggar, YS; Elsheikh, MA; Gohar, EY, 2012
)
0.38
" A self-microemulsifying drug delivery system (SMEDDS) has been developed to enhance the solubility and oral bioavailability of oleanolic acid."( Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation.
Dou, J; Huang, X; Su, L; Yang, R; Zhai, G, 2013
)
0.39
"BCS class III hydrophilic compounds are often associated with low oral bioavailability due to their poor epithelial permeability in the gastrointestinal tract."( Enhanced bioavailability of poorly absorbed hydrophilic compounds through drug complex/in situ gelling formulation.
Dai, WG; Dong, LC; Song, Y, 2013
)
0.39
"2-fold improved oral bioavailability of leuprolide oleate SMEDDS compared to a leuprolide acetate control solution."( In vivo evaluation of an oral self-microemulsifying drug delivery system (SMEDDS) for leuprorelin.
Bernkop-Schnürch, A; Hauptstein, S; Hintzen, F; Laffleur, F; Müller, C; Perera, G, 2014
)
0.4
" γ-T3 incorporated in SEDDS or Tocovid was orally administered to rats at different doses and absolute oral bioavailability from both formulations were determined."( Enhanced solubility and oral bioavailability of γ-tocotrienol using a self-emulsifying drug delivery system (SEDDS).
Alayoubi, A; Alqahtani, S; Kaddoumi, A; Nazzal, S; Sylvester, PW, 2014
)
0.4
"Microemulsions show significant promise for enhancing the oral bioavailability of biopharmaceutics classification system (BCS) class II drugs, but how about class III drugs remains unclear."( Improving oral bioavailability of metformin hydrochloride using water-in-oil microemulsions and analysis of phase behavior after dilution.
Cai, J; Hu, H; Huang, M; Li, Y; Song, J; Tian, N; Wang, Y; Wu, C; Xing, Q, 2014
)
0.4
"5% poloxamer 188 group, with absolute bioavailability 29."( Non-ionic surfactants as novel intranasal absorption enhancers: in vitro and in vivo characterization.
Ding, J; Li, J; Li, Y; Mao, S; Zhang, X, 2016
)
0.43
"The aim of this study was to examine the efficacy of self-nano phospholipid dispersions (SNPDs) based on Phosal(®) to improve the oral bioavailability of curcumin (CUR)."( Preparation, characterization and in vivo evaluation of curcumin self-nano phospholipid dispersion as an approach to enhance oral bioavailability.
Abdallah, OY; Allam, AN; Fouda, MA; Komeil, IA, 2015
)
0.42
"Itraconazole (ITR), an antifungal agent has poor bioavailability due to low aqueous solubility."( Formulation and evaluation of Itraconazole nanoemulsion for enhanced oral bioavailability.
Dhande, RD; Khunt, A; Patel, AA; Thakkar, HP, 2015
)
0.42
"Oral emodin, a natural anthraquinone and active component of many herbal medicines, is poorly bioavailable because of extensive first-pass glucuronidation."( Cremophor EL-based nanoemulsion enhances transcellular permeation of emodin through glucuronidation reduction in UGT1A1-overexpressing MDCKII cells.
Dong, D; Lu, D; Wang, S; Wu, B; Zhang, T, 2016
)
0.43
"Efflux transporters are extensively distributed and expressed in the intestinal epithelium and contribute to the low oral bioavailability of flavonoids and flavonoid glucuronides by pumping these compounds back into intestinal lumen."( A new mechanism for increasing the oral bioavailability of scutellarin with Cremophor EL: Activation of MRP3 with concurrent inhibition of MRP2 and BCRP.
Chen, M; Lam, CW; Xiao, L; Yi, T; Zhou, H, 2016
)
0.43
" The low oral bioavailability is a great challenge for oral formulation development."( Novel oral administrated paclitaxel micelles with enhanced bioavailability and antitumor efficacy for resistant breast cancer.
Ding, R; Fu, Y; Gong, T; Li, H; Luo, J; Zhang, T; Zhang, Z, 2017
)
0.46
"The goal of the present investigation was to improve ATV bioavailability and overcome complications attendant with peroral administration by developing a new nanovesicular system encapsulating ATV for its delivery via the transdermal route."( Transdermal delivery of atorvastatin calcium from novel nanovesicular systems using polyethylene glycol fatty acid esters: Ameliorated effect without liver toxicity in poloxamer 407-induced hyperlipidemic rats.
Aboud, HM; Ali, AA; Hassan, AH; Johnston, TP; Mahmoud, MO, 2017
)
0.46
" However, the use of paclitaxel is seriously limited (its bioavailability is <10%) due to several long-standing challenges: its poor water solubility (0."( Basic principles of drug delivery systems - the case of paclitaxel.
Aserin, A; Ezrahi, S; Garti, N, 2019
)
0.51
"The purpose of this study was to use hydroxypropyl-β-cyclodextrin (HP-β-CD) as a novel carrier in solid SNEDDS and solid dispersions to enhance the solubility and oral bioavailability of poorly water-soluble dexibuprofen."( New potential application of hydroxypropyl-β-cyclodextrin in solid self-nanoemulsifying drug delivery system and solid dispersion.
Cheon, S; Choi, HG; Choi, YJ; Im, D; Ji, SH; Jin, SG; Kim, JO; Kim, JS; Lim, SJ; Oh, KT; Ud Din, F; Woo, MR; Youn, YS, 2021
)
0.62

Dosage Studied

Cremophor EL (polyethoxylated castor oil) is a likely etiology for this acute adverse reaction. Paclitaxel dissolved either in ethanol or ethanol plus cremophorEL resulted in steep and almost identical dose-response curves for the parental lines ZR 75-1 and HS 578T.

ExcerptRelevanceReference
" Because of the drug's poor water solubility, ethoxylated plant fats and ethanol are added to the commercially available dosage forms."( Dosage forms of cyclosporine.
Yee, GC, 1991
)
0.28
" The presence of Cremophor EL as an emulsifying agent in the parenteral dosage formulation of cyclosporine is a likely etiology for this acute adverse reaction."( Anaphylactoid reactions associated with parenteral cyclosporine use: possible role of Cremophor EL.
Burckart, GJ; Griffith, BP; Hardesty, RJ; Howrie, DL; Ptachcinski, RJ; Rosenthal, JT; Venkataramanan, R, 1985
)
0.27
" Paclitaxel dissolved either in ethanol or ethanol plus cremophor EL, resulted in steep and almost identical dose-response curves for the parental lines ZR 75-1 and HS 578T, respectively, independent of the solvent used."( Paclitaxel-induced cytotoxicity--the effects of cremophor EL (castor oil) on two human breast cancer cell lines with acquired multidrug resistant phenotype and induced expression of the permeability glycoprotein.
Bergh, J; Fjällskog, ML; Frii, L, 1994
)
0.29
" Exposure times and dose-response relationships should be explored to optimize future clinical applications of this drug."( Analysis of exposure times and dose escalation of paclitaxel in ovarian cancer cell lines.
Adler, LM; Herzog, TJ; Mutch, DG; Rader, JS; Williams, S, 1994
)
0.29
" dosage form of PSC 833, [3'-keto-Bmt1]-[Val2]-cyclosporin, contains CreEL and has been presumed to have the potentiation of the reversal activity of PSC 833."( Cremophor EL reversed multidrug resistance in vitro but not in tumor-bearing mouse models.
Itoh, Y; Naito, M; Nakayama, Y; Oh-hara, T; Tsuruo, T; Watanabe, T, 1996
)
0.29
" An aqueous acetonitrile (ACN) buffer containing sodium dodecyl sulfate (SDS) surfactant allows resolution of the 15 taxanes from each other and from the principal matrix ingredient in the injectable dosage form of the drug, Cremophor EL (polyethoxylated castor oil)."( Separation of paclitaxel and related taxanes by micellar electrokinetic capillary chromatography.
Locke, DC; Shao, LK, 1998
)
0.3
"Paclitaxel's optimal dosage and scheduling is currently not determined."( Cell line and schedule-dependent cytotoxicity of paclitaxel (Taxol): role of the solvent Cremophor EL/ethanol.
Cordes, N; Plasswilm, L,
)
0.13
" The compound is pharmaceutically formulated as a lyophilized product containing 500 microg active substance per dosage unit."( Compatibility and stability of aplidine, a novel marine-derived depsipeptide antitumor agent, in infusion devices, and its hemolytic and precipitation potential upon i.v. administration.
Beijnen, JH; Bouma, M; Bult, A; Henrar, RE; Manada, C; Nuijen, B, 1999
)
0.3
" The pharmaceutical formulation consists of a lyophilized product containing 150 micrograms kahalalide F, 3 mg citric acid, 3 mg polysorbate 80, and 150 mg of sucrose per dosage unit, to be reconstituted with 3 mL of a mixture composed of Cremophor EL, ethanol, and water (5/5/90% v/v/v), resulting in a solution of pH 3 and to be further diluted in normal saline for infusion."( In vitro hemolysis and buffer capacity studies with the novel marine anticancer agent kahalalide F and its reconstitution vehicle cremophor EL/ethanol.
Beijnen, JH; Bouma, M; Bult, A; Jimeno, JM; Manada, C; Nuijen, B,
)
0.13
" Kahalalide F is pharmaceutically formulated as a lyophilized product containing 150 microg active substance per dosage unit."( Compatibility and stability of the investigational polypeptide marine anticancer agent kahalalide F in infusion devices.
Beijnen, JH; Bouma, M; Bult, A; Jimeno, JM; Lazaro, LL; Manada, C; Nuijen, B, 2001
)
0.31
" dosing (17."( Influence of Cremophor El on the bioavailability of intraperitoneal paclitaxel.
Buijs, D; Gelderblom, H; Nooter, K; Ouwens, L; Sparreboom, A; Stoter, G; van Zomeren, DM; Verweij, J, 2002
)
0.31
" For this purpose, the fractionating robot Probot was employed which enables both the on-line fractionation of the CE eluate on a MALDI target during the electrophoretic separation and the simultaneous dosage of the MALDI matrix solution."( Separation and first structure elucidation of Cremophor EL-components by hyphenated capillary electrophoresis and delayed extraction-matrix assisted laser desorption/ionization-time of flight-mass spectrometry.
Frahm, AW; Meyer, T; Waidelich, D, 2002
)
0.31
" Clinically relevant peripheral neurotoxicity tended to occur at around 1500 mg/m2 cumulative dosage at weekly doses > or =110 mg/m2."( Pharmacodynamics of non-break weekly paclitaxel (Taxol) and pharmacokinetics of Cremophor-EL vehicle: results of a dose-escalation study.
Briasoulis, E; Haidou, C; Karavasilis, V; Pavlidis, N; Piperidou, C; Tzamakou, E, 2002
)
0.31
" In order to combine CE and MS the fractionating robot Probot was employed which enables both the online fractionation of the CE eluate on a MALDI target during the electrophoretic separation and the simultaneous dosage of the MALDI matrix."( Polyoxyethylene-Delta(9,11)-didehydrostearate and glycerol-polyoxyethylene-Delta(9,11)-didehydrostearate: two new components of the non-ionic emulsifier Cremophor EL.
Frahm, AW; Meyer, T; Waidelich, D, 2002
)
0.31
" The purpose of this study was to use a rat model to evaluate whether the pharmacokinetic interaction between OPT and PXL is dosing sequence-dependent."( Dosing sequence-dependent pharmacokinetic interaction of oxaliplatin with paclitaxel in the rat.
Balcerzak, S; Chan, KK; D'Ambrosio, S; Grever, M; Kraut, EH; Liu, J, 2002
)
0.31
" The 24-h urinary elimination of total Pt increased in both combination groups, irrespective of the dosing sequence."( Dosing sequence-dependent pharmacokinetic interaction of oxaliplatin with paclitaxel in the rat.
Balcerzak, S; Chan, KK; D'Ambrosio, S; Grever, M; Kraut, EH; Liu, J, 2002
)
0.31
"These results suggest that alterations in the pharmacokinetics of OPT by fPXL are dosing sequence-dependent and mainly caused by the formulation vehicle CrEL."( Dosing sequence-dependent pharmacokinetic interaction of oxaliplatin with paclitaxel in the rat.
Balcerzak, S; Chan, KK; D'Ambrosio, S; Grever, M; Kraut, EH; Liu, J, 2002
)
0.31
"The aim of this study was to systematically obtain a model of factors that would yield an optimized self-nanoemulsified capsule dosage form (SNCDF) of a highly lipophilic model compound, Coenzyme Q10 (CoQ)."( Response surface methodology for optimization and characterization of limonene-based coenzyme Q10 self-nanoemulsified capsule dosage form.
Khan, MA; Nutan, MT; Palamakula, A, 2004
)
0.32
" The incidence of grade 3 sensory neuropathy was higher in nab-paclitaxel recipients, reflecting the higher dosage of nab-paclitaxel, and improved with treatment interruption."( Albumin-bound Paclitaxel: in metastatic breast cancer.
Keating, GM; Robinson, DM, 2006
)
0.33
") to the desired drug dosing concentration at the acceptable excipient level."( Solubilization and preformulation of poorly water soluble and hydrolysis susceptible N-epoxymethyl-1,8-naphthalimide (ENA) compound.
Dong, Y; Ng, WK; Surana, U; Tan, RB, 2008
)
0.35
" The droplet size and dissolution of optimal formulation were determined to prove that the dosage form is a useful delivery system for piroxicam."( [Design and in vitro evaluation of self-microemulsifying drug delivery systems for piroxicam].
Nie, SF; Pan, WS; Sun, JY; Wang, J; Wang, Y; Zhou, XT, 2008
)
0.35
" Development of a novel semimechanistic pharmacodynamic model permitted quantitative hypothesis testing with the tumor volume progression data, and suggested the existence of a transient treatment effect that was consistent with sensitization or "priming" of tumors by more frequent L-pac dosing schedules."( Differential pharmacodynamic effects of paclitaxel formulations in an intracranial rat brain tumor model.
Harrold, JM; Mager, DE; Mazurchuk, RV; Straubinger, RM; Tamburlin, JH; Zhou, R, 2010
)
0.36
"To compare physiochemical properties of mono-, di- and triglycerides of medium chain fatty acids for development of oral pharmaceutical dosage forms of poorly water-soluble drugs using phase diagrams, drug solubility, and drug dispersion experiments."( A comparative evaluation of mono-, di- and triglyceride of medium chain fatty acids by lipid/surfactant/water phase diagram, solubility determination and dispersion testing for application in pharmaceutical dosage form development.
Dalrymple, DM; Prajapati, HN; Serajuddin, AT, 2012
)
0.38
" Emodin transport and metabolism were evaluated in Transwell-cultured MDCK1A1 cells after apical dosing of EMO-NE or control solution."( Cremophor EL-based nanoemulsion enhances transcellular permeation of emodin through glucuronidation reduction in UGT1A1-overexpressing MDCKII cells.
Dong, D; Lu, D; Wang, S; Wu, B; Zhang, T, 2016
)
0.43
" Accordingly, ML-SNEP coated with Kollicoat Smartseal 30D and/or silicon dioxide could be an excellent dosage form that combine dual enhancement of CN solubilization and stabilization."( Stabilization benefits of single and multi-layer self-nanoemulsifying pellets: A poorly-water soluble model drug with hydrolytic susceptibility.
Abdel-Rahman, SI; Alanazi, FK; Shahba, AA, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (380)

TimeframeStudies, This Drug (%)All Drugs %
pre-199038 (10.00)18.7374
1990's101 (26.58)18.2507
2000's120 (31.58)29.6817
2010's114 (30.00)24.3611
2020's7 (1.84)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials24 (6.02%)5.53%
Reviews15 (3.76%)6.00%
Case Studies12 (3.01%)4.05%
Observational0 (0.00%)0.25%
Other348 (87.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]