中文摘要：

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一聚天冬氨酸苄酯（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^-1（P〈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。

英文摘要：

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.