Polysaccharide-based aerogel microspheres for oral drug delivery
Polysaccharide-based aerogel microspheres for oral drug delivery
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DOI：
10.1016/j.carbpol.2014.10.045
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发表时间：
2015-03-06
影响因子：
11.2
通讯作者：
Smirnova, I.
中科院分区：
文献类型：
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作者：
Garcia-Gonzalez, C. A.;Jin, M.;Smirnova, I.
以微球形式的多糖气凝胶作为难溶口服药物的载体进行了研究。这些生物载体可能结合了多糖的生物相容性和增强的干气凝胶的载药能力。由淀粉、果胶和海藻酸盐制成的气凝胶微球通过超临界CO2辅助吸附负载了酮洛芬(抗炎药)和苯甲酸(用于尿素循环障碍的治疗)。载药量取决于气凝胶基质的结构和组成，酮洛芬和苯甲酸在淀粉微球中的载药量分别达到1.0×10~(-3)和1.7×10~(-3)g/m~(2)。经浸渍后，药物在气凝胶微球中处于无定形状态。考察其在不同pH介质(pH 1.2和6.8)中的释药行为。果胶和海藻酸盐气凝胶微球的药物控释符合Gallagher-Corrigan释放模型(R-2和0.99)，不同基质组成对溶蚀和扩散机制的相对贡献不同。淀粉气凝胶微球的释放受溶解驱动，符合一级动力学，释放速率常数k(I)因药物不同而不同(酮洛芬和苯甲酸的释放速率常数分别为0.075和0.160 m in-1)。总体而言，这些结果指出了通过仔细选择用于制备气凝胶的多糖来调节药物载量和释放的可能性。(C)2014爱思唯尔有限公司。保留所有权利。
Polysaccharide-based aerogels in the form of microspheres were investigated as carriers of poorly water soluble drugs for oral administration. These bio-based carriers may combine the biocompatibility of polysaccharides and the enhanced drug loading capacity of dry aerogels. Aerogel microspheres from starch, pectin and alginate were loaded with ketoprofen (anti-inflammatory drug) and benzoic acid (used in the management of urea cycle disorders) via supercritical CO2-assisted adsorption. Amount of drug loaded depended on the aerogel matrix structure and composition and reached values up to 1.0 x 10(-3) and 1.7 x 10-3 g/m(2) for ketoprofen and benzoic acid in starch microspheres. After impregnation, drugs were in the amorphous state in the aerogel microspheres. Release behavior was evaluated in different pH media (pH 1.2 and 6.8). Controlled drug release from pectin and alginate aerogel microspheres fitted Gallagher-Corrigan release model (R-2 >0.99 in both cases), with different relative contribution of erosion and diffusion mechanisms depending on the matrix composition. Release from starch aerogel microspheres was driven by dissolution, fitting the first-order kinetics due to the rigid starch aerogel structure, and showed different release rate constant (k(i)) depending on the drug (0.075 and 0.160 min(-1) for ketoprofen and benzoic acid, respectively). Overall, the results point out the possibilities of tuning drug loading and release by carefully choosing the polysaccharide used to prepare the aerogels. (C) 2014 Elsevier Ltd. All rights reserved.