Dastinib nasosponges-formulation development and evaluation

Annapurna Tippareddy, V. J. Marabathuni, Naidu Narapusetty
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Abstract

Nanosponges of Dasatinib were prepared by the solvent evaporation technique by employing Ethyl Cellulose,  β Cyclodextrin, and poloxamer as rate retarding polymers using PVA as a copolymer.  however, at higher ratios, drug crystals were observed on the nanosponge surface. An increase in the drug/polymer ratio (1:3 to 1:1) is in increasing order due to the increase in the concentration of polymer. However, after a particular concentration, it was observed that as the ratio of Drug to polymer was increased, the particle size decreased. The particle size was found in the range of 250- 450 nm. The entrapment efficiency of different formulations was found in the range of 90.56 to 98.32%, by comparing the above dissolution studies of formulations F1-F9. Maximum drug release was found in the F5 formulation containing Drug: β-cyclodextrin in a 1:3 ratio. So F5 formulation was taken as the optimized formulation, and drug release kinetics were performed and which follows zero-order kinetics with super case II transport mechanism.
达替尼鼻海绵-配方开发与评价
以乙基纤维素、β环糊精和波洛沙姆为缓速聚合物,聚乙烯醇为共聚物,采用溶剂蒸发法制备达沙替尼纳米海绵。然而,在较高的比例下,在纳米海绵表面观察到药物晶体。随着聚合物浓度的增加,药物/聚合物比(1:3 ~ 1:1)的增加呈递增趋势。然而,在一定浓度后,观察到随着药物与聚合物比例的增加,颗粒尺寸减小。粒径在250 ~ 450 nm之间。通过对配方f1 ~ f9的溶出度研究,发现不同配方的包封效率在90.56 ~ 98.32%之间。药物与β-环糊精比例为1:3的F5制剂释放量最大。以F5处方为优化处方,进行药物释放动力学研究,其释放动力学符合零级动力学,具有超病例转运机制。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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