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目的:本文目的是制备氟维司群纳米聚合物胶束,并对其体外特性进行表征。方法:采用生物可降解材料甲氧基聚乙二醇-b-聚D,L-丙交酯(m PEG-b-PDLLA),并用固体分散法制备氟维司群聚合物胶束。利用透射电子显微镜与马尔文激光粒度测定仪分析胶束的形态与粒径。用X射线单晶体衍射仪定性测试胶束包封性。建立并验证氟维司群高效液相色谱(HPLC)分析方法,定量测定胶束载药量与包封率。采用透析袋法分析胶束体外释放情况。结果:氟维司群聚合物胶束形态圆整、分散均匀无粘连,粒径为89.97±4.33 nm,多分散指数为0.162±0.023,载药量与包封率达8.95%±0.86%与97.25%±0.86%。胶束释药具有明显的缓释特点。结论:成功制备氟维司群胶束并显著提高其水溶性,表现良好的缓释行为,能够开发为氟维司群的新型纳米制剂。
Objective: The purpose of this paper is to prepare fulvestrant nano-polymer micelles, and to characterize its in vitro characteristics. Methods: The bi-degradable material methoxypolyethylene glycol-b-poly D, L-lactide (m PEG-b-PDLLA) was prepared and the fulvestrant micelles were prepared by solid dispersion method. Morphology and particle size of micelles were analyzed by transmission electron microscopy and Malvern laser particle sizer. Characterization of Micelle Encapsulation by X - ray Single Crystal Diffractometer. To establish and validate fulvestrant high performance liquid chromatography (HPLC) analysis method for the quantitative determination of drug loading and entrapment efficiency of micelles. Analysis of micellar in vitro release by dialysis bag method. Results: The fulvestrant micelles were round and uniformly dispersed without particles, the particle size was 89.97 ± 4.33 nm, polydispersity index was 0.162 ± 0.023, drug loading and encapsulation efficiency reached 8.95% ± 0.86% and 97.25 % ± 0.86%. Micelle release has a significant slow release characteristics. Conclusion: The successful preparation of fulvestrant micelles and significantly improve its water-soluble, good performance of sustained-release behavior, can be developed as fulvestrant nano-formulations.