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  

Preparation of Polymer Drug-loading Micelles of Saponin Rb1 Active Metabolite NG701 and in Vitro Cytotoxicity Evaluation

作　　者：朱宇轩[1] 贾乙[1] 张建祥[1] 李晓辉[1] 

机构地区：[1]第三军医大学药剂学教研室,重庆市400038

出　　处：《中国药房》2011年第17期1576-1579,共4页China Pharmacy

基　　金：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。OBJECTIVE： To prepare polymer drug-loading micelles of Rbl 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 as the model to evaluate the cytotoxicity of NG701-1oading PEG-PBLA micelles by MTT assay. It was compared with that of NG701 raw material. RESULTS： IR spectrum and HNMR confirmed the synthesis of PEG-PBLA. Prepared micelles were in round shape with size smaller than 200 nm. The drug-loading rate reached 32.7% at the most and encapsulation coefficency was 93.2% at the most. Compared with active concentration of NG701 raw material 100 μg. mL^-1, the active concentration of polymer was 50 μg. mL^-1（P〈0.05）. CONCLUSION： Polymer drug-loading micelles with PEG-PBLA as carrier can improve cytotoxicity of NG 701 effectively.

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 

分 类 号：R943[医药卫生—药剂学] R965[医药卫生—药学]