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蛋白微球作为吡罗昔康释放的合适载体。

Protein microspheres as suitable devices for piroxicam release.

机构信息

University of Minho, Department of Textile Engineering, Campus de Azurém, Guimarães, Portugal.

出版信息

Colloids Surf B Biointerfaces. 2012 Apr 1;92:277-85. doi: 10.1016/j.colsurfb.2011.11.050. Epub 2011 Dec 8.

Abstract

Bovine serum albumin-piroxicam (BSA-piroxicam) and human serum albumin-piroxicam (HSA-piroxicam) microspheres were sonochemically prepared and characterized. The use of polyvinyl alcohol (PVA) lead to an improvement of formulation characteristics, including smaller size, lower polydispersity index (PDl), higher entrapment efficiency and higher stability. The release kinetics of these proteinaceous microspheres was determined in presence of protease, indicating an anomalous drug transport mechanism (diffusion and polymer degradation). In presence of higher protease concentration, BSA microspheres exhibit Case II transport, leading to zero order release (protein degradation). These proteinaceous devices did not show cytotoxicity against human skin fibroblasts in vitro, for range concentrations below to 300 mg L(-1), greatly supporting their potential application in the treatment of inflammatory diseases.

摘要

牛血清白蛋白-吡罗昔康(BSA-吡罗昔康)和人血清白蛋白-吡罗昔康(HSA-吡罗昔康)微球经声化学法制备并进行了表征。使用聚乙烯醇(PVA)可改善制剂特性,包括粒径更小、多分散指数(PDl)更低、包封效率更高、稳定性更高。在存在蛋白酶的情况下,测定了这些蛋白质微球的释放动力学,表明存在异常的药物传递机制(扩散和聚合物降解)。在较高蛋白酶浓度下,BSA 微球表现出 II 型转运,导致零级释放(蛋白降解)。这些蛋白质装置在体外对人皮肤成纤维细胞没有细胞毒性,在浓度低于 300mg/L 的范围内,极大地支持了它们在治疗炎症性疾病方面的潜在应用。

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