| 范迎方 庄波 杨双 徐雪莲 刘堂荣 宋清平 殷加奇 王成.氟维司群纳米聚合物胶束的制备与表征[J].现代生物医学进展英文版,2016,16(7):1219-1223. |
| 氟维司群纳米聚合物胶束的制备与表征 |
| Preparation and Characterization of Fulvestrant Polymeric Nanomicelles |
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| DOI： |
| 中文关键词: 氟维司群 聚合物胶束 固体分散法 体外释放 |
| 英文关键词: Fulvestrant Polymeric micelle Solid dispersion method In vitro release |
| 基金项目:中央高校基本科研业务专项（201413066）；中国博士后科学基金项目（2014M561969）；
山东省科技发展计划项目（2014GGH215001）；国家自然科学基金-山东省政府联合资助项目（U1406402）；
山东省自然科学基金项目（ZR2012HQ017） |
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| 中文摘要: |
| 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（mPEG-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。 |
| 英文摘要: |
| Objective:The purpose of this article is to prepare the fulvestrant nanomicelles (FNM) and investigate its physicochemical
properties in vitro.Methods:FNMwas made up of biodegradable mPEG-b-PDLLA copolymer and was prepared by solid dispersion
method. The morphology and particle size of FNM was investigated by transmission electron microscopy (TEM) and malvern
laser particle size analyzer. The characters were detected by and X-ray diffraction (XRD). High-performance liquid chromatography
(HPLC) analysis method was built and verified, using to measure drug loading and encapsulation efficiency. A dialysis method was used
to determine the in vitro release behaviors of FNM.Results:The micelles are well dispersed as individual nanoscaled micelles with regularly
spherical shape. The particle size and polydisperse index of FNMwere 89.97± 4.33 nm and 0.162± 0.023, respectively. Drug loading
and encapsulation efficiency reached 8.95 %± 0.86 %and 97.25 %± 0.86 %. FNM exhibited sustained-release action in vitro.Conclusion:The mPEG-b-PDLLA micelles loaded fulvestrant were successfully prepared. In vitro experiments showed that FNM significantly
enhanced solubility of fulvestrant and released fulvestrant at a controlled rate. FNM should hold great potential for developing a
novel formulation. |
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