瑞德西韦聚合物纳米胶束的制备及表征  

Preparation and characterization of Remdesivir Polymeric Nanomicelles

作　　者：武海军 李玉凤[2] 钟强 张广桃 马春雷 谢纪珍 WU Haijun;LI Yufeng;ZHONG Qiang;ZHANG Guangtao;MA Chunlei;XIE Jizhen(Shandong Center for Food and Drug Evaluation and Inspection,Jinan 250013,China;Qingdao Municipal Hospital,Qingdao 266033,China;Shandong Hubble Kisen Biological Technology Co.,Ltd.,Jinan 250098,China)

机构地区：[1]山东省食品药品审评查验中心,山东济南250013 [2]青岛市市立医院,山东青岛266033 [3]山东华铂凯盛生物科技有限公司,山东济南250098

出　　处：《药学研究》2022年第3期165-170,共6页Journal of Pharmaceutical Research

基　　金：山东省重点研发计划(重大科技创新工程)(No.2019JZZY021014)。

摘　　要：目的改良瑞德西韦现有剂型,构建瑞德西韦聚合物纳米胶束,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瑞德西韦聚合物胶束。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裹效果,并通过高效液相色谱(HPLC)方法定量测定胶束载药量与包封率,采用透析袋法考察胶束体外释放情况。结果瑞德西韦聚合物纳米胶束形态圆整、分散均匀无黏连,粒径为(12.97±1.33)nm,多分散指数为(0.062±0.023),载药量与包封率分别为(10.95%±0.33%)与(99.25%±0.86%),且具有较好的缓释特性。结论成功制备瑞德西韦聚合物纳米胶束,显著提高其水溶性,具有较好的缓释行为,具有开发瑞德西韦新型纳米制剂的潜力。Objective To prepare the Remdesivir Nanomicelles(RNM)and investigate its physico-chemical properties in vitro.Methods RNM was made up of biodegradable mPEG-b-PDLLA copolymer and was prepared by solid dis-persion method.The morphology and particle size of RNM was investigated by transmission electron microscopy(TEM)and Malvern laser particle size analyzer.The characters including drug loading and encapsulation efficiency were detected by X-ray diffraction(XRD)and High-performance liquid chromatography(HPLC).A dialysis method was used to determine the in vitro release behaviors of RNM.Results The micelles are well dispersed as individual nanoscale micelles with regularly spherical shape.The particle size and polydisperse index of RNM were(12.97±1.33)nm and(0.062±0.023),respectively.Drug loading and encapsulation efficiency reached(10.95%±0.33%)and(99.25%±0.86%).RNM exhibited sustained-release action in vitro.Conclusion The mPEG-b-PDLLA micelles loaded remdesivir were successfully prepared.In vitro experiments showed that RNM significantly enhanced solubility of remdesivir and released remdesivir at a controlled rate.RNM should hold great potential for developing a novel formulation.

关 键 词：瑞德西韦 聚合物胶束 固体分散法 体外释放 

分 类 号：R943[医药卫生—药剂学]