目的 制备盐酸伊立替康胶束给药系统,降低其毒副作用,提高治疗效果。方法 首先将盐酸伊立替康制备成磷脂复合物,提高其脂溶性;以合成的聚己内酯-聚乙二醇共聚物作为载体材料,将盐酸伊立替康磷脂复合物包裹其中,制备聚合物胶束给药系统。单因素结合正交试验,筛选制备盐酸伊立替康胶束给药系统的最佳处方和制备工艺。结果 盐酸伊立替康磷脂复合物与原药相比脂溶性显著增加;制得的盐酸伊立替康胶束呈球形,粒径分布较均匀,包封率平均为61.32%,载药量平均为2.88%。结论 通过该方法制得的盐酸伊立替康胶束粒径较小、质量可控,有望提高靶向部位药物浓度。

OBJECTIVE To prepare micelle drug delivery system of irinotecan hydrochloride, which could reduce its side effects and improve the therapeutic effects.METHODS Firstly, the irinotecan hydrochloride was prepared as phospholipid compound to improve the lipophilicity. The synthesized polycaprolactone-polyethylene glycol copolymer was used as carrier material, then the phospholipid complex of irinotecan hydrochloride was wrapped to prepare a polymer micelle drug delivery system. The optimum prescription and preparation process of micelle drug delivery system of irinotecan hydrochloride were screened by the method of single factor combined with orthogonal test.RESULTS The liposoluble of phospholipid compound of irinotecan hydrochloride was obviously increased compared with active compound. The irinotecan hydrochloride micelle was spherical and its particle size distribution was uniform. The average entrapment efficiency was 61.32%, and the average drug loading was 2.88%.CONCLUSION Through this method, the particle size of irinotecan hydrochloride is small and the quality is controllable, and it is hopeful to increase the drug concentration at the target site.