【摘要】 构建荷载紫杉醇的普朗尼克F127-聚乙烯亚胺聚合物/胆酸钠聚电解质复合物胶束,然后将其包载到脂质体中增加稳定性,并对其理化性质和对癌细胞的杀灭能力进行考察。采用薄膜法制备紫杉醇聚电解质复合物胶束,以载药量为指标筛选最佳处方。然后将其包裹到脂质体中,并对粒径、Zeta电位、微观形态、载药量、体外释放进行测定。以多药耐药人乳腺癌细胞(MCF-7/Adr)为模型,考察荷载紫杉醇脂质体的细胞毒性。紫杉醇脂质体的粒径为125.5 nm,Zeta电位为-4.05 mV,载药量为(5.83±0.78)%,脂质体外观圆整,基本没有粘连。相比紫杉醇游离药物,脂质体具有明显控制释放的特点。细胞毒性结果显示,相比游离药物脂质体具有更好地杀灭癌细胞的能力。荷载紫杉醇的脂质体具有较高的载药量和较强地杀灭癌细胞的能力,是一种比较理想的药物释放系统。更多还原

【Abstract】 In this study,novel paclitaxel(PTX) loaded hybrid liposomes for PTX delivery were prepared.During the process,the author incorporated PTX loaded polyion complex micelles comprised of positively charged Pluronic F127-Polyethylenimine(PF127-PEI) copolymer and negatively charged sodium cholate(CA) into liposomes consisted of phospholipid molecules.After that,investigating loaded into liposomes increased stability and its physicochemical properties as well as the ability to kill cancer cells.The paclitaxel loaded polyelectrolyte complex micelles were produced by film method after a detailed comparison between many kinds of methods.The optimal formulation was obtained,during the process,the drug loading content was deemed as one of the key indexes.After the previous steps,the particle size,Zeta potential,morphology,drug loading content and in vitro release were then determined.Following that step,multidrug-resistant human breast cancer cells(MCF-7/Adr) were taken as model,studying the cytotoxicity of the paclitaxel-loaded liposomes.All the experimental results show that liposomes have better ability to kill cancer cells than free drug.At same time,results showed that the spherical micelles have an average diameter of 125.5 nm,and Zeta potential of-4.05 m V.Drug loading capacity(DL%) was about 5.83%.After a careful observation,it was found that the cells had a round appearance,and there was almost no adhesion.Compared with paclitaxel free drug,liposomes have the characteristics of obvious controlled release.What is more,the author made an experiment related to cytotoxicity,and the results showed that compared with free drug liposomes,the new ones had a better ability to kill cancer cells.In vitro release study suggested that PTX-loaded hybrid liposomes exhibited a sustained drug release.More important,PTX-loaded hybrid liposomes demonstrated a superior cytotoxicity against MCF-7/Adr to PTX solution.Liposomes loaded with paclitaxel had high drug loading and strong ability to kill cancer cells,PTX-loaded hybrid liposomes were a kind of potential drug delivery system for PTX.更多还原