Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan, China.
Drug Dev Ind Pharm. 2013 May;39(5):662-9. doi: 10.3109/03639045.2012.687378. Epub 2012 May 21.
Objective of this study was to prepare, characterize and evaluate a self-microemulsifying drug delivery system (SMEDDS) with the aim to improve the solubility and dissolution of apigenin. Ternary phase diagrams were constructed in order to obtain the most efficient self-emulsification region, and the formulation of apigenin loaded SMEDDS was optimized by a simplex lattice experiment design. The optimal formulation of SMEDDS obtained was comprised of 60% Cremophor(®)EL, 30% Transcutol(®)HP and 10% Capryol™ 90. The equilibrium solubility of apigenin in SMEDDS was about 15 mg/g, and it could increase the solubility of apigenin in water for about 7500 folds. Apigenin loaded SMEDDS could turn into microemulsion when diluted with distilled water and the droplets were spherical under transmission electron microscope (TEM), the average particle size was 17.1 nm and zeta potential -5.18 mV. In vitro dissolution studies showed about 95% of apigenin was released within 10 min. All of the results showed that SMEDDS could enhance the solubility and dissolution of apigenin, and would be a potential carrier to improve the oral absorption of apigenin, a poorly water soluble drug.
本研究的目的是制备、表征和评价一种自微乳药物传递系统（SMEDDS），旨在提高芹菜素的溶解度和溶解速率。通过构建三元相图来获得最有效的自乳化区域，并通过单纯形格子实验设计对载有芹菜素的 SMEDDS 配方进行优化。所得 SMEDDS 的最佳配方由 60%的 Cremophor®EL、30%的 Transcutol®HP 和 10%的 Capryol™90 组成。SMEDDS 中芹菜素的平衡溶解度约为 15mg/g，可将芹菜素在水中的溶解度提高约 7500 倍。载有芹菜素的 SMEDDS 用蒸馏水稀释后可转化为微乳，在透射电子显微镜（TEM）下观察到液滴呈球形，平均粒径为 17.1nm，zeta 电位为-5.18mV。体外溶解研究表明，约 95%的芹菜素在 10 分钟内释放。所有结果表明，SMEDDS 可以提高芹菜素的溶解度和溶解速率，有望成为一种提高难溶性药物芹菜素口服吸收的潜在载体。
