载吡非尼酮的丙烯酰胺接枝普鲁兰-聚乙烯醇互穿聚合物网络的体外和体内评价。
In vitro and in vivo evaluation of pirfenidone loaded acrylamide grafted pullulan-poly(vinyl alcohol) interpenetrating polymer networks.
机构信息
Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, 835215, Jharkhand, India.
Biomaterial and Tissue Engineering Laboratory, Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Guwahati 781039, Assam, India.
出版信息
Carbohydr Polym. 2018 Dec 15;202:288-298. doi: 10.1016/j.carbpol.2018.08.135. Epub 2018 Aug 31.
The aim of present study was to develop controlled release formulation of pirfenidone using acrylamide grafted pullulan. Interpenetrating polymer network (IPN) microspheres were prepared using acrylamide grafted pullulan and PVA utilizing glutaraldehyde assisted water-in-oil emulsion crosslinking method. IPN microspheres were characterized by FTIR, solid state C NMR and XRD spectroscopy. In vitro enzymatic degradation study showed 34.30% degradation after 24 h with degradation rate constant of 0.0088 min. In vitro biocompatibility test showed no changes in cellular morphology and cell adherence to microspheres, indicating its biocompatible nature. The release exponent value of all formulations was less than 0.45, indicating the release mechanism to be Fickian diffusion. Finally, in vivo pharmacokinetic study showed longer T (1.16 h) and greater AUC value (10037.76 ng h/mL,) as compared to Pirfenex (T = 0.5 h; AUC = 4310.45 ng h/mL,). The results indicated that the prepared formulation could successfully control the drug release for prolonged time period.
本研究旨在开发使用丙烯酰胺接枝普鲁兰的吡非尼酮控释制剂。采用丙烯酰胺接枝普鲁兰和 PVA，利用戊二醛辅助的油包水乳液交联法制备互穿聚合物网络（IPN）微球。通过傅里叶变换红外光谱（FTIR）、固态 C NMR 和 XRD 光谱对 IPN 微球进行了表征。体外酶降解研究表明，24 小时后降解了 34.30%，降解速率常数为 0.0088 min。体外生物相容性试验表明，微球对细胞形态和细胞黏附没有影响，表明其具有生物相容性。所有制剂的释放指数值均小于 0.45，表明释放机制为菲克扩散。最后，体内药代动力学研究表明，与吡非尼酮（T = 0.5 h；AUC = 4310.45 ng h/mL）相比，该制剂具有更长的 T（1.16 h）和更大的 AUC 值（10037.76 ng h/mL）。结果表明，所制备的制剂能够成功地控制药物释放，延长释放时间。
Zotero 插件