Formulation Development, Physicochemical Characterization and In Vitro-In Vivo Drug Release of Vaginal Films.

PURPOSE: The purpose of this study was formulation and optimization of vaginal film formulation containing abacavir (ABC), a potent nucleoside reverse transcriptase inhibitor. METHODS: Vaginal films were prepared by solvent evaporation method using hydroxypropyl methylcellulose (HPMC) blended with polyvinyl pyrrolidone (PVP). Various physicochemical parameters of the prepared films such as drug content, thickness, tensile strength, percentage elongation at break, drug polymer interaction, swelling capacity, folding endurance, bio-adhesion, pH, and moisture content were evaluated with morphological studies. In vitro release study and in vivo release study were also performed. RESULTS: Films exhibited favorable physicochemical properties. The in vitro study showed that HPMC-PVP combination can control the release of abacavir through vaginal films with higher amount of PVP in the formulation resulting in an enhanced drug release rate. During the in vivo study in rabbits, systemic absorption of the drug was noted and the films remained intact for long in vagina without causing any sort of irritations. CONCLUSION: Thus, in a nutshell, the findings of our experimental work indicate that such films can be considered as a novel drug carrier system for the treatment of AIDS and other sexually transmitted diseases (STDs), and are suitable for local as well as systemic effects.

Pharmacokinetic evaluation of testosterone-loaded nanocapsules in rats.

In the present work, testosterone-loaded alginate nanocapsules were prepared by in situ nanoemulsification-polymer cross-linking method. Drug loading, particle size (diameter), polydispersity index and zeta potential of these alginate nanocapsules were measured 30.22 ± 1.90%, 34.53 ± 1.72 nm, 0.22 ± 0.04 and -5 mV, respectively. The pharmacokinetic evaluation of these nanocapsules was also performed in female Sprague Dawley rats. Cmax, Tmax and AUC0-24 vales were estimated 38.63ng/ml, 2h and 317.93 ng ml(-1) h(-1), respectively. The pharmacokinetic result of testosterone-loaded alginate nanocapsules indicates better bioavailability in comparison with pure testosterone and commercial testosterone injection.

A novel vaginal drug delivery system: anti-HIV bioadhesive film containing abacavir.

Women are very much susceptible for acquired immunodeficiency syndrome (AIDS) and other sexually transmitted diseases (STDs), mainly due to unprotected heterosexual vaginal intercourse and for some other social and economical disadvantages. Our aim was to formulate and optimize vaginal film of abacavir, a potent nucleoside reverse transcriptase inhibitor, for the treatment of AIDS and HIV. Abacavir films were prepared by solvent evaporation method using sodium alginate (Na-alginate) as the main polymer, Hydroxypropyl Methylcellulose E 15 (HPMC E 15) as the copolymer and glycerol as a humectant. Abacavir sulphate (ABC) was used here as a drug. Films were optimized for various physicochemical parameters such as tensile strength, % elongation at break, swelling capacity, drug content (mg/cm(2)), thickness, folding endurance, bioadhesion, pH, moisture content and SEM. Drug polymer interaction was studied by FTIR Spectra. The drug release study was accomplished in dissolution apparatus. In vivo study was also carried out. This newly formed film was one kind of sustain release type and can be considered as a novel drug carrier system for the treatment of AIDS and other STDs. It was suitable for local as well as systemic effect. The films showed good physicochemical property with good aesthetic appeal.

Microparticulated anti-HIV vaginal gel: in vitro-in vivo drug release and vaginal irritation study.

The aim of this study was to develop and evaluate a Zidovudine (AZT)-loaded microparticulated bioadhesive vaginal gel (MBVG) in order to obtain a controlled releasing, safe gel delivery system. AZT microparticles (ZMPs) were evaluated for encapsulation efficiency, drug loading, surface morphology and in vitro drug release profiles and drug release mechanism and optimized. The optimized ZMPs were then encompassed in bioadhesive gel using different bioadhesive polymers and evaluated for the drug encapsulation efficiency, drug loading, in vitro and in vivo drug release profiles, drug release mechanism and vaginal irritancy study. From the dissolution data of ZMP4 and MBVG4 showed a zero-order diffusion pattern and Fickian diffusion case I transport mechanism in 24 and 36 h, respectively. On the basis of a pharmacokinetic study of MBVG4 (containing ZMP: Carbopol 1:4), it was found to have better bioavailability, larger AUC and T(max) in comparison to an oral pure suspension of AZT.

Preparation and in vitro characterization of slow release testosterone nanocapsules in alginates.

Slow release testosterone-loaded nanocapsules in alginate, biodegradable hydropolymer, were prepared by in situ nanoemulsion-polymer crosslinking approach. Different formulations varying in the drug loading solvent phase were prepared. Four different drug-loading solvents were assayed and the food grade hexane provided nanocapsules testosterone load of 30%. Testosterone loading was confirmed by FT-IR, DSC and quantitated by HPLC. Prepared nanocapsules appeared spherical with a dense drug core in transmission electron microscopy studies. Hydrodynamic diameter of nanocapsules was 34.5 +/- 1.7 nm, with a Gaussian distribution and the zeta potential -5.0 meV. Sustained diffusive drug release was observed in vitro, following zero order kinetics releasing the drug payload over a period of 48 hours. Embedding testosterone in alginate provided sustained release. Different drug loading solvents have distinct influence on drug loading and nanocapsules size distribution. The nanocapsulation technique developed can be a good choice for the development of different sustained steroid hormonal drug carriers.