SN-38脂质体的制备及质量评价的研究

Study on preparation and quality evaluation of SN-38 liposomes

目的探究7-乙基-10-羟基喜树碱(SN-38)脂质体的最佳制备方法并进行相关制剂学评价研究。方法采用薄膜分散法制备羟基喜树碱脂质体,选用高效液相色谱法进行测定,以包封率和载药量为相关的评价指标,在单因素考察下优化相关制备工艺并进行质量评价初探。结果制备工艺中,药物和磷脂质量比为1:20,胆固醇用量为20%,水化温度为60℃,包封率平均值为(91.28±3.27)%,载药量为(3.65±0.21)%,选择质量分数为10%的蔗糖为保护剂,制备SN-38脂质体的冻干品;质量评价方面,SN-38脂质体的外观为淡蓝色近澄明溶液,平均粒径为145±23 nm,粒度分布D90/D10=1.5,相关粒径均呈现均一的单峰分布,脂质体在3 h内总释药量均不超过12%。结论选用薄膜分散法制备羟基喜树碱脂质体的工艺操作简便、合理可行。

Objective To explore the best preparation method of 7-ethyl-10-hydroxycamptothecin(SN-38)liposomes and to conduct related pharmaceutics evaluation research.Methods The hydroxycamptothecin liposomes were prepared by the thin film dispersion method and determined by high performance liquid chromatography.The encapsulation efficiency and drug loading were used as the relevant evaluation indicators,and the relevant preparation process and quality were optimized under single factor investigation.Results In the preparation process,the mass ratio of drug and phospholipid was 1:20,the amount of cholesterol was 20%,the hydration temperature was 60℃,the average encapsulation efficiency was(91.28±3.27)%,and the drug loading was(3.65±0.21)%.The 10%mass fraction of sucrose was selected as the protective agent to prepare the freeze-dried product of SN-38 liposomes;The appearance of SN-38 liposomes was a light blue nearly clear solution with an average particle size of(145±23)nm.The particle size distribution of D90/D10 was 1.5,the relevant particle sizes all presented a uniform unimodal distribution,and the total drug release amount of liposomes within 3 h did not exceed 12%.Conclusion The process of preparing hydroxycamptothecin liposomes by the film di spersion method is simple,reasonable and feasible.