Zhang Ji-Fen, Hou Shi-Xiang, Liu Hui-Lian
School of Pharmacy, Southwest University, Chongqing 400715, China.
Zhongguo Zhong Yao Za Zhi. 2007 Feb;32(4):303-6.
This paper introduced an experimental study of polylacticacid (PLA) nanoparticles of lipophilic anti-cancer herb drug using a precipitation method. Cucurbitacins (Cu) and Curcuminoids (Cur) were selected to be model drugs. They had similar solubility but their incorporation effects were significantly different: the average drug entrapment ratio, the average drug loading and the average drug recovery were 38.53%, 2.21% and 27.02% respectively; while those of Cur-PLA-NP were 94.36%, 14.35% and 91.23% respectively. To analyse the reason, drug incorporation process was investigated. By measuring solvent evaporation rate, ratio of drug PLA precipitates, drug distribution in system and entrapping ratio at different time of preparation, we found the difference of precipitation velocity of drug was the main reason. We also concluded that not all lipophilic drug can be well entrapped into PLA nanoparticle by nanoprecipitation method. The drug incorporation depended on the interations among drug, PLA and organic solvents, in addition to the solubility of the drug.
本文介绍了采用沉淀法对亲脂性抗癌草药药物聚乳酸(PLA)纳米颗粒进行的实验研究。选择葫芦素(Cu)和姜黄素(Cur)作为模型药物。它们具有相似的溶解度,但它们的包封效果却有显著差异:平均药物包封率、平均载药量和平均药物回收率分别为38.53%、2.21%和27.02%;而Cur-PLA-NP的相应数值分别为94.36%、14.35%和91.23%。为分析原因,对药物包封过程进行了研究。通过测量溶剂蒸发速率、药物-PLA沉淀物的比例、体系中药物的分布以及制备不同时间的包封率,我们发现药物沉淀速度的差异是主要原因。我们还得出结论,并非所有亲脂性药物都能通过纳米沉淀法很好地包封到PLA纳米颗粒中。药物包封除了取决于药物的溶解度外,还取决于药物、PLA和有机溶剂之间的相互作用。