For improving bioavailability in controlled release fashion and to circumvent the hepatic first pass effect of glipizide mucoadhesive buccal films of glipizide were prepared by solvent casting technique. Buccal films were prepared using hydroxy propylmethylcellulose, sodium carboxymethylcellulose, carbopol-934P and Eudragit RL-100. Films were evaluated for their weight, thickness, surface pH, swelling index, in vitro residence time, folding endurance, in vitro release, ex vivo permeation studies and drug content uniformity. The films exhibited controlled release over more than 6 h. From the study it was concluded that the films containing 5 mg glipizide in 4.9 % w/v hydroxy propylmethylcellulose and 1.5 % w/v sodium carboxymethylcellulose exhibited satisfactory swelling, an optimum residence time and promising drug release thus proved to be potential candidate for the development of buccal films for therapeutic use.
A group of novel heterocyclic arylsulfonamide derivatives were synthesized by three steps process using the organic and inorganic catalyst in less solvent at ambient temperature. One out of the three-steps process, one-pot multiple component reaction using the reusable organic catalyst. These compounds reactions proceed through Knoevenagel condensation accompanied by Michael addition to obtaining suspicious products. The synthesized compound's structure was characterized by spectral data (UV-vis, FTIR and 1 H-NMR). Subsequently, the obtained novel final products are "benzoxazole clubbed chromene aryl sulfonamide derivatives". The green synthesis process was used to obtain optimum yield products to fulfil the required conditions such as nontoxic, inexpensive, minimum solvent and reusable catalyst.
Objective: The present study has focused on development and optimization of thermosensitive in-situ ocular drug delivery system for the treatment of conjunctivitis.Methods: Thermosensitive in-situ hydrogel formulation of moxifloxacin hydrochloride was developed by dispensing variable concentration of pluronic F-127, gellan-gum, and carbopol in distilled water. Viscosity, gelation temperature and mean release time (MRT) were measured by using ‘Brookfield' viscometer LV-III (spindle no. 40), rheological techniques and dissolution apparatus respectively. Optimization for ideal formulation was carried by ‘Box–Behnken' design on the basis of prime factors of the formulation including viscosity, gelation temperature, and MRT. Moreover, the optimized formulation was evaluated for accelerated stability study by in vitro drug release, anti-microbial potential by ‘Kirby-Bauer disk diffusion' method and ocular irritancy assay were done by in vivo analysis.Results: Optimised thermosensitive in-situ gel, when administered into cul-de-sac region of the eye, it was immediately transformed from sol to gel by multi-dimensional mechanism due to plurionic, gellan-gum, carbopol. The optimized formulation minimizes the chances of formulation failure as well as the concentration on individual polymer which dependence on a single mechanism of gelation. The final optimised formulation consists of plurionic (11.50% w/v), gellan-gum (0.32% w/v), carbopol (0.3% w/v), shows optimum therapeutic effect. Moreover, the accelerated stability study, anti-microbial potential, and ocular irritancy confirmed the biocompatibility of optimized in-situ drug-containing gel with high potency and stability.Conclusion: Thus, optimized in-situ drug-containing gel with multifactorial approaches showed promising ocular formulation having minimum side effect and high therapeutic efficacy.Â
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