Morphology and release kinetics of protein-loaded porous poly(l-lactic Acid) spheres prepared by freeze-drying technique.

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-08-15 DOI:10.5402/2011/490567
Takashi Sasaki, Kazuki Tanaka, Daisuke Morino, Kensuke Sakurai
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引用次数: 2

Abstract

Freeze-drying a biodegradable polymer, poly(L-lactic acid) (PLLA), from 1,4-dioxane solutions provided very porous spherical particles of ca. 3 mm in radius with specific surface area of 8-13 m(2) g(-1). The surface of the particle was found to be less porous compared with its interior. To apply the freeze-dried PLLA (FDPLLA) to drug delivery system, its morphology and drug releasing kinetics were investigated, bovine serum albumin (BSA) being used as a model drug compound. Immersion of FDPLLA into a BSA aqueous solution gave BSA-loaded FDPLLA, where mass fraction of the adsorbed BSA reached up to 79%. Time-dependent release profile of BSA in water suggested a two-step mechanism: (1) very rapid release of BSA deposited on and near the particle surface, which results in an initial burst, and (2) leaching of BSA from the interior of the particle by the diffusion process. It was suggested that the latter process is largely governed by the surface porosity. The porosity of both the interior and surface was found to decrease remarkably as the concentration of the original PLLA/1,4-dioxane solution increases, C(0). Thus, C(0) is a key parameter that controls the loading and releasing of BSA.

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冷冻干燥法制备载蛋白多孔聚乳酸微球的形貌及释放动力学。
从1,4-二氧六环溶液中冷冻干燥生物可降解聚合物聚l -乳酸(PLLA),可提供半径约3 mm的多孔球形颗粒,比表面积为8-13 m(2) g(-1)。人们发现,这种颗粒表面的多孔性比其内部要少。以牛血清白蛋白(BSA)为模型药物化合物,研究了冻干PLLA (FDPLLA)的形态和释药动力学。将FDPLLA浸泡在BSA水溶液中得到负载BSA的FDPLLA,其吸附的BSA质量分数高达79%。BSA在水中的时间依赖性释放曲线表明,BSA在水中的释放机制分为两步:(1)沉积在颗粒表面及其附近的BSA快速释放,导致初始爆发;(2)BSA通过扩散过程从颗粒内部浸出。结果表明,后一过程在很大程度上受表面孔隙率的控制。随着原始PLLA/1,4-二氧六环溶液浓度的增加,内部和表面的孔隙率均显著降低,C(0)。因此,C(0)是控制BSA加载和释放的关键参数。
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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