[关键词]
[摘要]
目的 制备两亲性聚合物β-环糊精-聚乙二醇-7-乙基-10-羟基喜树碱(β-CD-PEG-SN38)纳米胶束并进行质量评价。方法 采用自组装法制备β-CD-PEG-SN38纳米胶束,采用单因素变量法对影响纳米胶束粒径的因素进行了考察,并对β-CD-PEG-SN38纳米胶束的粒径、Zeta电位、形态和稳定性进行评价。结果 胶束制备的最佳条件为丙酮作有机溶剂,β-CD-PEG-SN38在丙酮中的质量浓度为1 mg/mL,有机相和水相的体积比为1∶8。该纳米胶束大小适中、粒径分布均匀,为均匀的球形结构。β-CD-PEG-SN38纳米胶束的临界胶束质量浓度为7 μg/mL,在模拟的生理条件下具有良好的胶体稳定性,在4℃条件下储存6个月的粒径未发生明显变化。结论 β-CD-PEG-SN38在水中能自发形成纳米胶束,粒径均匀、稳定性好,具有良好的胶体稳定性和长期储存稳定性。
[Key word]
[Abstract]
Objective To prepare β-cyclodextrin-polyethylene glycol-7-ethyl-10-hydroxycamptothecin nanomicelle and evaluate the quality. Methods β-CD-PEG-SN38 micelle was prepared in water with the self-assembly method. The single factor variable method was used to investigate the factors affecting the particle size of nanomicelles. The properties of β-CD-PEG-SN38 micelle were evaluated, including particle size, Zeta potential, appearance, and stability. Results The optimal conditions for preparation of β-CD-PEG-SN38 micelle were optimized. Acetone was used as the organic solvent, the concentration of β-CD-PEG-SN38 in acetone was 1 mg/mL, and the volume ratio of organic phase to aqueous phase was 1:8. The micelle displayed a moderate size, uniform particle size distribution, and a uniform spherical structure. The critical micelle concentration of β-CD-PEG-SN38 nanomicelles was 7 μg/mL, and it had good colloidal stability under simulated physiological conditions. The particle size of 6-month storage at 4℃ did not change significantly. Conclusion The particle size distribution ofβ-cyclodextrin-polyethylene glycol-7-ethyl-10-hydroxycamptothecin nanomicelle is uniform, and it has good colloidal stability and long-term storage stability.
[中图分类号]
R963
[基金项目]
南昌市科技重大项目重大科技攻关项目(15);江西中医药大学“1050青年人才工程”项目(5142001006);江西中医药大学校级研究生创新专项资助项目(JZYC20S05)