betadex and carboxypolymethylene

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also, in vitro skin permeation of LOR was conducted. The effect of hydroxypropyl β-cyclodextrin (HP β-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm(2)/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HP β-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HP β-CD and may be promising in enhancing permeation.

Topics: Acrylic Resins; Administration, Cutaneous; Animals; beta-Cyclodextrins; Calorimetry, Differential Scanning; Humans; Hydrogen-Ion Concentration; Male; Piroxicam; Rabbits; Skin; Skin Absorption; Viscosity

This study focuses on the development of amlodipine bilayer buccal tablets of hydroxypropyl methylcellulose (HPMC) matrix system containing polyacrylate polymer (Carbopol(®))/β-cyclodextrin as the drug layer and ethylcellulose as the non-swellable backing layer, and their biointerfacial phenomena.. Tablets were evaluated for swelling, erosion and mucoadhesion using buccal mucosal tissue ex vivo. In vitro drug release and ex vivo drug transport across mucosal tissue were also performed in phosphate buffer (pH 6.8). The relationship of swelling with buccoadhesion and buccal permeation of various bilayer tablet formulations containing HPMC alone and in combination with Carbopol or drug-β-cyclodextrin complex has been prepared.. Overall buccoadhesion of the tablet with combination of HPMC and Carbopol was increased significantly compared with that of HPMC alone. Presence of cyclodextrin did not change bioadhesion force and swelling behavior significantly. Ex vivo permeation was increased with the increase of HPMC proportion in other formulations as observed in in vitro dissolution.. Drug-cyclodextrin complexes in the tablet improved permeation due to its improved dissolution at the site of biointerface of tablet and buccomucosa. Correlations of ex vivo and in vitro data have been established to predict the buccomucosal permeation from the swelling index or drug release alone.

Topics: Acrylic Resins; Administration, Buccal; Amlodipine; Animals; beta-Cyclodextrins; Biological Transport; Calcium Channel Blockers; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Drug Delivery Systems; Lactose; Male; Methylcellulose; Mouth Mucosa; Sheep; Spectroscopy, Fourier Transform Infrared; Tablets

Supramolecular cyclodextrin (CD) hydrogels have occupied an important position in developing the materials for biomedical application. In the present work an attempt has been made to improve the release profile of ciprofloxacin by designing the β- cyclodextrin containing drug delivery system through network formation and supramolecular interactions. The polymer network has been formed by sterculia gum comprising of glucuronic acid and galacturonic acid and carbopol. The polymers have been characterization by cryo-SEMs, FTIR and

Topics: Acrylic Resins; Animals; Antioxidants; beta-Cyclodextrins; Carbon-13 Magnetic Resonance Spectroscopy; Ciprofloxacin; Cryoelectron Microscopy; Delayed-Action Preparations; Drug Delivery Systems; Drug Liberation; Goats; Humans; Hydrogels; Hydrogen-Ion Concentration; Spectrophotometry, Ultraviolet; Spectroscopy, Fourier Transform Infrared; Temperature

A novel mucoadhesive buccal patch formulation of triclosan (TR), a broad spectrum antibacterial agent, was developed using low methoxy amidated pectin (AMP). The integrity of AMP matrix was improved by addition of 20% (w/w) Carbopol (CAR). The efficiency of β-cyclodextrin-epichlorohydrin polymer (EPIβCD) and anionic carboxymethylated β-cyclodextrin-epichlorohydrin polymer (CMEPIβCD) in optimization of TR solubility and release from such a matrix was investigated and confronted to that of parent β-cyclodextrin (βCD). Loading of TR/βCD co-ground complex into AMP/CAR matrix resulted in a biphasic release profile which was sensitive upon the hydration degree of the matrix, due to lower solubilizing efficiency of βCD, while the drug release from patches loaded with TR/EPIβCD complex was significantly faster with a constant release rate. Microbiological studies evidenced faster onset and more pronounced antibacterial action of TR/EPIβCD loaded patches, clearly demonstrating their good therapeutic potential in eradication of Streptococcus mutans, a cariogenic bacteria, from the oral cavity.

Topics: Acrylic Resins; Adhesiveness; Administration, Buccal; Amides; Animals; Anti-Infective Agents, Local; beta-Cyclodextrins; Cheek; Drug Carriers; Drug Delivery Systems; Mouth Mucosa; Pectins; Permeability; Polyvinyls; Streptococcus mutans; Swine; Triclosan

The purpose of this study was to investigate the nasal absorption of progesterone from carbopol-based nasal gels in rabbits. Progesterone nasal gels were prepared by dispersing carbopol 974 (1%, 1.5%, and 2%) in distilled water followed by addition of progesterone/progesterone-beta cyclodextrin complex dissolved in propylene glycol then neutralization. The potential use of beta cyclodextrin (CD) as nasal absorption enhancer by simple addition, as a physical mixture and as a complex with progesterone was investigated. The absolute bioavailability of progesterone from nasal gels in rabbits was studied by estimating the serum progesterone level by competitive solid-phase enzyme immunoassay in comparison to intravenous injection. The carbopol gel formulations produced a significant increase in bioavailability. CD complex promotes the nasal absorption of progesterone from carbopol gels as compared with gels where the CD is added by simple addition and gels which do not contain CD. This method of addition of CD as an inclusion complex in the gels could be considered as a preferred platform in nasal drug administration.

Topics: Acrylic Resins; Administration, Intranasal; Animals; Area Under Curve; beta-Cyclodextrins; Biological Availability; Calorimetry, Differential Scanning; Drug Carriers; Gels; Immunoenzyme Techniques; Polyvinyls; Progesterone; Rabbits; Spectroscopy, Fourier Transform Infrared

We evaluated the ability of hydroxypropyl-beta-cyclodextrin (HPbetaCD) to influence the percutaneous absorption of capsaicin (CP) through isolated rat skin. Phase solubility analysis and phase distribution studies suggested the potential of HPbetaCD as a solubilizer and permeation enhancer for CP. In vitro permeation studies showed the trend that, the penetration flux (J(s)) of CP increased with the increasing concentration of HPbetaCD from 0 to 2.20% (w/v), and then decreased dramatically when the concentration of HPbetaCD kept on increasing up to 15% (w/v). 2.20% (w/v) of HPbetaCD provided both just adequate solubilization and preferred J(s) for the permeation of CP (0.075%, w/v). Similar change patterns of the permeation parameters were also observed in the hydrogels, but the J(s) of CP was reduced significantly along with the increasing concentration of Carbopol U21. Histological analysis showed an invasive action of HPbetaCD on the stratum corneum (SC) of rat skin, which could only reduce the lag time (T(L)) but could not increase the J(s) of CP. On the other hand, the complexation of HPbetaCD with CP could attenuate this invasive action. It is inferred that excess of HPbetaCD could not only disturb the percutaneous absorption of CP but also disrupt the structure of SC.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Acrylic Resins; Administration, Cutaneous; Animals; beta-Cyclodextrins; Calorimetry, Differential Scanning; Capsaicin; Chromatography, High Pressure Liquid; Excipients; Female; Freeze Drying; Hydrogels; In Vitro Techniques; Male; Microscopy, Electron, Transmission; Pharmaceutical Solutions; Polyvinyls; Rats; Rats, Sprague-Dawley; Skin Absorption; Solubility; Suspensions; X-Ray Diffraction

The purpose of this study was to develop a pH-triggered in situ gelling vehicle for ophthalmic delivery of puerarin. The effect of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) on the aqueous solubility and in vitro corneal permeation of puerarin was also investigated. The puerarin solubility increased linearly and proportionally to the HP-beta-CD concentrations and 5% (w/v) HP-beta-CD enhanced its ocular permeability significantly. Carbopol 980NF was used as the gelling agent in combination with HPMC (Methocel E4M) which acted as a viscosity-enhancing agent. The optimum concentrations of Carbopol 980NF and HPMC E4M for the in situ gel-forming delivery systems were 0.1% (w/v) and 0.4% (w/v), respectively. When these two vehicles were combined, an in situ gel that had the appropriate gel strength and gelling capacity under physiological condition could be obtained. This combined solution could flow freely under non- physiological condition and showed the character of pseudoplastic fluid under both conditions. Both in vitro release studies and in vivo pharmacokinetics studies indicated that the combined polymer systems performed better in retaining puerarin than puerarin eye drops did. These results demonstrate that the Carbopol 980NF/HPMC E4M can be a viable alternative to conventional puerarin eye drops to enhance ocular bioavailability and patient compliance.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Acrylic Resins; Animals; beta-Cyclodextrins; Biological Availability; Cell Membrane Permeability; Cornea; Drug Carriers; Drug Delivery Systems; Female; Gels; Hydrogen-Ion Concentration; Hypromellose Derivatives; In Vitro Techniques; Isoflavones; Male; Methylcellulose; Ophthalmic Solutions; Polymers; Polyvinyls; Rabbits; Solubility; Vasodilator Agents; Viscosity

The aim of the present study was to design a new mucosal drug delivery system composed of liposomes dispersed within a bioadhesive hydrogel containing methyl-beta-cyclodextrin (Me(beta)CD) for controlled drug release.. A hydrophilic model molecule, inulin, was encapsulated within positively charged and PEG-ylated liposomes and its release was measured in the presence of Me(beta)CD after vesicle dispersion within the bioadhesive Carbopol 974P gel. Freeze-fracture electron microscopy (FFEM) was used to follow liposome morphological changes when dispersed within the hydrogel. Liposome-Me(beta)CD interactions were investigated by turbidity monitoring during continuous addition of Me(beta)CD to liposomes and by FFEM.. Inulin diffusion within the gel was influenced by Carbopol 974P concentration since no gel erosion occurred. When dispersed within the gel, positively charged liposomes displayed a higher stability than PEG-ylated vesicles. In the presence of Me(beta)CD, higher amounts of free inulin were released from liposomes, especially in Carbopol-free system. Me(beta)CD appeared to diffuse towards lipid vesicles and permeabilized their bilayer allowing inulin leakage. Indeed, freeze-fracture experiments and liposome turbidity monitoring have shown that Me(beta)CD behaved as a detergent behavior, resulting in lipid vesicle solubilization.. is able to mediate, within a bioadhesive hydrogel, the release of a liposome-encapsulated molecule allowing further application of this delivery system for mucosal administration.

Topics: Acrylic Resins; Adhesives; beta-Cyclodextrins; Chemical Phenomena; Chemistry, Physical; Drug Compounding; Freeze Fracturing; Freezing; Gels; Inulin; Lipid Bilayers; Liposomes; Microscopy, Electron; Nephelometry and Turbidimetry; Pharmaceutical Preparations; Polyvinyls; Solubility

A modified release bi-layered tablet of melatonin incorporating a fast release fraction consisting of melatonin-beta-cyclodextrin inclusion complex and a slow release fraction containing melatonin in HPMC K15M and Carbopol 971 P matrices was prepared. The formulation developed showed an initial burst followed by a near zero order release pattern for a period of 8 h. The drug content, physical characteristics and the release profile were unaffected after 3 months of an accelerated stability study at 40 degrees C and 75% relative humidity.

Topics: Acrylic Resins; Antioxidants; beta-Cyclodextrins; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Cyclodextrins; Delayed-Action Preparations; Drug Stability; Excipients; Kinetics; Lactose; Melatonin; Methylcellulose; Microscopy, Electron, Scanning; Oxazines; Polyvinyls; Solubility; Spectroscopy, Fourier Transform Infrared; Tablets

Carbomers are carboxyvinylic derivatives that are widely used in the manufacture of hydrogel dosage forms. Because of their anionic nature and large number of acid groups, they tend to interact with cationic substances, and with other hydrophilic polymers containing alcohol groups. Here, we report a study of interactions between the carbomer Carbopol and the cationic drug propranolol hydrochloride in the solid state and in solution, and of the effects of such interactions on the properties of the hydrogel. We found that the drug forms an insoluble ionic complex with the polymer, modifying all of the hydrogel properties studied (swelling, release, bioadhesion). The inclusion of beta-cyclodextrin in the formulation reduces polymer/drug interactions, so that hydrogel properties remain unchanged. This is probably attributable to formation of inclusion complexes of beta-cyclodextrin and the drug, so that the drug is prevented from interacting with the polymer.

Topics: Acrylic Resins; beta-Cyclodextrins; Cyclodextrins; Dosage Forms; Drug Carriers; Drug Incompatibility; Hydrogels; Kinetics; Polymers; Polyvinyls; Propranolol; Solutions; Temperature; Time Factors

The in vivo ocular bioavailability of hydrocortisone (HC) in the NZW rabbit was determined following topical administration of solutions containing HC (1%) with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) alone, or containing the mucoadhesive, viscosity enhancing polymers sodium hyaluronate (0.2 and 0.5% w/v) or Carbopol 934P (0.1% w/v). A 1% HC suspension was used as control. Formulation of HC as a solution with HP-beta-CD in the absence of polymer increased the bioavailability of HC in the aqueous humour by approximately 55% and cornea by 75% when compared to suspension. Inclusion of either polymer did not result in any further increase in ocular bioavailability over that noted for the polymer-free solution. The in vitro corneal permeability of HC was also evaluated. A linear relationship (r(2)=0.999) was noted between corneal permeability and the concentration of free (uncomplexed) HC in solution. Permeability was greatest when formulated either as a suspension, or as an HP-beta-CD solution in which the concentration of free (uncomplexed) HC is equivalent to that of a saturated solution. Thus, when using cyclodextrins in the reformulation of ophthalmic suspensions as solutions, consideration must be given to the concentration of cyclodextrin used and to the benefits of including viscosity enhancing polymers.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Acrylic Resins; Animals; beta-Cyclodextrins; Biological Availability; Chemistry, Pharmaceutical; Cyclodextrins; Eye; Hydrocortisone; Ophthalmic Solutions; Permeability; Polyvinyls; Rabbits; Swine

The aim of this work was to study the cross-linkage of xerogels made of Carbopol of different molecular weight (polymers deriving from polyacrylic acid), and the influence exerted by different percentages of beta-cyclodextrin upon the cross-linkage percentage. Xerogels were obtained by high-pressure compression and cross-linking was studied by measuring the weight loss of different formulations over a temperature range of 70 to 190 degrees C. Kinetics of anhydride formation were found to follow a second-order mechanism with an activation energy of approximately 25 kcal mol-1.

Topics: Acrylic Resins; Anhydrides; beta-Cyclodextrins; Calorimetry, Differential Scanning; Cross-Linking Reagents; Cyclodextrins; Drug Carriers; Gels; Kinetics; Mathematics; Molecular Weight; Polyvinyls

The bioconversion of (-)-drimenol [1] and drimenyl acetate [2] into the corresponding 3 beta-hydroxydrimanes by Aspergillus niger in agitated liquid cultures was investigated. Initial hydroxylation yields of 2% and 10%, respectively, were obtained. However, drimenyl acetate hydroxylation increased to 18% when Carbopol-934 was added. The highest transformation yield (33%) was reached when an inclusion complex of drimenyl acetate to beta-cyclodextrin (1:1 w/w) was added to the cultures, after 48 h of cultivation. The effect on growth and transformation yields of both additives is discussed.

Topics: Acrylic Resins; Aspergillus niger; beta-Cyclodextrins; Biotransformation; Cyclodextrins; Polyvinyls; Sesquiterpenes

The effect of the complexation with beta-cyclodextrin, hydroxypropyl beta-cyclodextrin and polyvinylpyrrolidone on the diffusion kinetics of hydrocortisone acetate through a non porous lipidic membrane was analyzed starting from different dermal bases: a Carbopol gel and lanovaseline. A constant diffusive gradient was achieved; this suggests that the complexation equilibrium controls the diffusable form, according to its stability constant. The following sequence was observed for the cumulative amount diffused: hydrocortisone acetate greater than hydrocortisone acetate/polyvinylpyrrolidone greater than hydrocortisone acetate/hydroxypropyl beta-cyclodextrin greater than hydrocortisone acetate/beta-cyclodextrin. Such behaviour was analyzed in terms of the main physical chemical parameters of the systems examined.

Topics: Acrylic Resins; Administration, Topical; beta-Cyclodextrins; Chemical Phenomena; Chemistry, Physical; Cyclodextrins; Diffusion; Hydrocortisone; Membranes, Artificial; Polyvinyls; Povidone; Silicone Elastomers