摘要
目的:探索沉淀法制备载药聚乳酸(PLA)纳米粒的过程,为沉淀法的合理应用奠定基础。方法:以脂溶性抗癌中药葫芦素(CuC)为模型药物,采用沉淀法制备其聚乳酸纳米粒,并详细考察制备过程中不同时刻的丙酮残留量、药物和载体的沉淀比例及其与包封效果的关系。结果:丙酮刚注入水相时,近60%的PLA包裹了5.5%的CuC形成纳米粒;随着丙酮的挥发,包载过程继续进行,但大部分的CuC(约70%)却形成了新晶核,以微晶形式存在于介质中,最终得到既有纳米粒又有微晶的混悬体系。结论:并非所有的脂溶性药物用沉淀法制备聚乳酸纳米粒都能得到高的包封率,包封效果除受药物溶解性能影响外,还可能与药物、载体、有机溶剂彼此间的作用强弱有关,选用时应慎重。
This paper introduced an experimental study of the preparation of polylacticacid (PLA) nanoparticles of cucurbitacin (CuC) using a precipitation method. The residual acetone, ratio of CuC- PLA precipitates, and the relationships between the ratios of two precipitates and drug incorporation rates were measured. It appeared that the nanoparticles with 60% of PLA incorporated with 5.5% of CuC were formed when acetone was injected into the aqueous phase. As the acetone gradually evaporated, drug incorporation/encapsulation continued, with most of CuC (about 70%) formed new crystalline cores and suspended in the form of microcrystals in the medium, resulting a suspension containing both nanoparticles and microcrystals. We also concluded that this system may not necessarily be suitable for all lipophilic drugs to be prepared to PLA nanoparticles with good incorporation rate. The drug incorporation depended on the interactions among drug, PLA, and organic solvents, in addition to the solubility of the drug.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2005年第6期436-439,共4页
China Journal of Chinese Materia Medica
