载甘草次酸的聚乙二醇-油酸胶束的制备及 制剂学研究  

Preparation and characterization of glycyrrhetinic acid-loaded polyethylene glycol-oleic acid micelles

作　　者：梁蔷薇 李莉[1] 刘艳华[1,2] LIANG Qiangwei;LI Li;LIU Yanhua(College of Pharmacy,Ningxia Medical University,Yinchuan 750004,Chian;Key Lab of Hui EthnicMedicine Modernization Ministry of Education,Yinchuan 750004,China)

机构地区：[1]宁夏医科大学药学院,宁夏银川750004 [2]回医药现代化省部共建教育部重点实验室,宁夏银川750004

出　　处：《广东药科大学学报》2020年第2期178-183,共6页Journal of Guangdong Pharmaceutical University

基　　金：宁夏高等学校科学研究项目(NGY2018-77)。

摘　　要：目的制备载甘草次酸(GA)的聚乙二醇-油酸(PEG-OA 2)聚合物胶束,并对该胶束进行制剂学研究。方法以聚乙二醇2000(PEG 2k)为亲水嵌段,与油酸(OA)发生接枝反应制备两亲性聚乙二醇-油酸(PEG-OA 2)聚合物,并研究其自组装特性;采用薄膜分散法制备载GA的聚合物胶束,并进行制剂学评价。结果合成的PEG-OA 2聚合物的临界胶束质量浓度为25.2μg/mL;空白胶束及PEG-OA 2与GA以摩尔比为1∶1、2.5∶1和5∶1制备的PEG-OA 2载药胶束的粒径分别为52.49、84.33、62.15、60.83 nm,GA的包封率依次是96.25%、92.47%和98.40%,GA的载药量分别为13.43%、5.63%和3.09%,且载药胶束可稳定长达7 d。结论制备的PEG-OA 2胶束载体对GA具有良好的包载能力及稳定性,可以作为包载难溶性药物的纳米载体。Objective The amphiphilic polyethylene glycol-oleic acid(PEG-OA 2)polymer micelles containing glycyrrhetinic acid(GA)were prepared,and these micelles were studied by pharmaceutics.Methods PEG-OA 2 amphiphilic carrier was prepared by grafting polyethylene glycol 2000(PEG 2k)as hydrophilic block with oleic acid(OA),and its self-assembly characteristic was studied.Polymer micelles containing GA were prepared by thin film dispersion method,and the characteristics of micelles were evaluated.Results The critical micelle concentration of the synthesized PEG-OA 2 polymer was 25.2μg/mL.The particle sizes of blank and GA loaded PEG-OA 2 micelles at molar ratios of PEG-OA 2 to GA with 1∶1,2.5∶1 and 5∶1 was 52.49 nm,84.33 nm,62.15 nm and 60.83 nm,respectively.The encapsulation efficiency of GA was 96.25%,92.47%and 98.40%,and the drug loading of GA was 13.43%,5.63%and 3.09%.The micelles loaded drug could stabilize for up to 7 d.Conclusion The PEG-OA 2 micelles have good loading ability and stability to GA,which can be used as nano-carrier for insoluble drugs.

关 键 词：聚乙二醇-油酸 甘草次酸 聚合物胶束 制备 制剂学研究 

分 类 号：R944.6[医药卫生—药剂学]