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皂苷Rb1活性代谢产物NG701聚合物载药胶束的制备及其体外细胞毒性评价
引用本文:朱宇轩,贾乙,张建祥,李晓辉. 皂苷Rb1活性代谢产物NG701聚合物载药胶束的制备及其体外细胞毒性评价[J]. 中国药房, 2011, 0(17): 1576-1579
作者姓名:朱宇轩  贾乙  张建祥  李晓辉
作者单位:第三军医大学药剂学教研室;
基金项目:国家自然科学基金资助项目(21004077)
摘    要:目的:制备二醇类皂苷Rb1活性代谢产物(NG701)的聚合物载药胶束,并对其进行体外细胞毒性评价。方法:合成两亲性嵌段共聚物即聚乙二醇-聚天冬氨酸苄酯(PEG-PBLA)并借助红外光谱和核磁共振氢谱进行表征;采用透析法制备NG701/PEG-PBLA聚合物载药胶束,观察其形态和粒径分布,建立高效液相色谱法测定其含量并计算载药量和包封率。以Hela细胞为模型,采用MTT法评价聚合物载药胶束的细胞毒性作用,并与NG701原料药比较。结果:红外光谱和核磁共振氢谱证实形成了PEG-PBLA,所制备的聚合物载药胶束呈球形,粒径小于200nm,载药量最高达32.7,包封率最高为93.2。与原料药发挥细胞毒性作用的有效浓度100μg.mL-1比较,聚合物载药胶束为50μg.mL-(1P<0.05)。结论:以PEG-PBLA为载体制备的载药胶束聚合物,可有效提高NG701的细胞毒性作用。

关 键 词:皂苷Rb1活性代谢产物  NG701  聚合物载药胶束  制备  体外细胞毒性

Preparation of Polymer Drug-loading Micelles of Saponin Rb1 Active Metabolite NG701 and in Vitro Cytotoxicity Evaluation
ZHU Yu-xuan,JIA Yi,ZHANG Jian-xiang,LI Xiao-hui. Preparation of Polymer Drug-loading Micelles of Saponin Rb1 Active Metabolite NG701 and in Vitro Cytotoxicity Evaluation[J]. China Pharmacy, 2011, 0(17): 1576-1579
Authors:ZHU Yu-xuan  JIA Yi  ZHANG Jian-xiang  LI Xiao-hui
Affiliation:ZHU Yu-xuan,JIA Yi,ZHANG Jian-xiang,LI Xiao-hui(Dept.of Pharmaceutics,The Third Military Medical University,Chongqing 400038,China)
Abstract:OBJECTIVE:To prepare polymer drug-loading micelles of Rb1 active metabolite(NG701),and to evaluate cytotoxicity of it in vitro.METHODS:Amphiphilic copolymer PEG-PBLA was synthesized and then characterized by IR spectrum and HNMR.Dialysis process was used to prepare NG701/PEG-PBLA polymer drug-loading micelles.The morphology and particle size of micelles were observed.The content of NG701 was determined by HPLC,and the drug-loading rate and encapsulation coefficency were calculated.Hela cells were employed a...
Keywords:Saponin Rb1 active metabolite  NG701  Polymer drug loading micelles  Preparation  In vitro cytotoxicity  
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