The aim of the present study is to formulate tenofovir loaded gelatin nanoparticles by two step desolvation method for targeted release of drug by varying the concentration of polymer and cross-linking agent. Entrapment efficiency for all the formulations was found to be within 67.32 ± 1.24 % to 92.11 ± 1.13 %. Average particle size of different tenofovir loaded gelatin nanoparticle formulations was found within the range of 294.9 -445.3 nm. In-vitro drug release study for glutaraldehyde cross linked gelatin nanoparticles were found between 67.09 % ± 1.423 -82.41 % ± 1.874 after 8 h of dissolution. F5 (850 mg gelatin, 0.2 ml glutaraldehyde) was considered as the best formulation based on the entrapment efficiency and drug release from nanoparticle core. Kinetics study was performed for all the formulations and best fit model for drug release was determined depending on R squared values. HPMC K15M was used as a bioadhesive polymer as well as a gelling agent. Three different gel formulations were prepared by varying concentration of HPMC K15M and incorporated with the best formulation, F5. Membrane permeation and bio-adhesion study revealed F5B gel (5% HPMC K15M) as an optimum formulation with suitable bioadhesive strength and membrane permeability.
Over the past few decades, chitosan (CS) has gained the attention of researchers investigating newer biomaterial-based carriers for drugs in pharmaceutical and biomedical research. Combined with its nontoxic behavior, biodegradability, and biocompatibility, chitosan has found widespread applications in the fields of drug delivery, tissue engineering, and cosmetics. As a novel drug carrier, chitosan is regarded as one of the promising biomaterials in the pharmaceutical industry. The extensive use of this cationic biopolysaccharide in the delivery of therapeutic agents has brought a few limitations of chitosan into the limelight. Various chemical modifications of chitosan can minimize these limitations and improve the efficacy of chitosan as a drug carrier. The effectiveness of several chemically modified chitosan derivatives, including trimethyl chitosan, thiolated chitosan, PEGylated chitosan, and other chitosan derivatives, has been investigated by many researchers for the controlled and target specific delivery of therapeutics. The chemically modified chitosan derivatives exhibited greater importance in the current scenario on drug delivery due to their solubility in wide range of media along with their interaction with pharmaceutically active ingredients. Chitosan derivatives have also attracted attention in several biomedical fields, including wound healing, hyperthermia therapy, tissue engineering, and bioadhesives. The present review narrates the sources and common physicochemical properties of chitosan, including several important synthetic modifications to obtain chemically modified chitosans and their applications in targetspecific drug delivery, along with several biomedical applications.
Objective: Tinidazole, a nitroimidazole derivative is having low aqueous solubility which is a major barrier for systemic drug absorption. The aim of the present research was to develop gastro retentive raft forming tablets of tinidazole to achieve prolonged gastric residence time and thus higher bioavailability.Methods: Solid dispersion of tinidazole was prepared by kneading method by using methanol and polyvinylpyrrolidone (PVP). Different concentration of sodium alginate and hydroxypropyl methylcellulose (HPMC) was used to formulate a suitable raft forming tablets and then evaluated for drug content, floating lag time, raft strength, raft volume, raft weight, drug release and release kinetics.Results: Fourier transform infra-red (FT-IR) study confirms compatibility between drug and polymer. The floating lag time was found in the range of 40±4 to 60±5 s for all the formulation. Raft strength for all the formulations was within the range from 3.03±0.12 to 5.92±0.06 g. The raft volume for all the formulation was found within the range of 7.37±1.86 to 9.84±2.76 ml. Raft weight was measured after completion of raft formation for each formulation and was found in the range of 5.21±1.17 to 7.88±1.95 g. In vitro dissolution was carried up to 8 h and percentage of drug release was found to vary between 79.71±2.18 to 94.32±1.79 %.
Conclusion:It can be concluded that the combination of solid dispersion and raft formation increases the bioavailability of tinidazole in tablet formulation.
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