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以二肽缬氨酸-瓜氨酸(VC)为连接片段合成了一种可酶降解的两亲性聚合物硬脂酸-缬氨酸-瓜氨酸-对氨基苯基碳酸酯-聚乙二醇甲醚(C18-VC-PABC-mPEG).该聚合物在水环境下可自组装形成粒径分布均一的球形胶束,平均粒径约179nm.通过模拟溶酶体条件研究其酶降解行为及其负载抗癌药物阿霉素(DOX)胶束的释药行为,发现聚合物胶束在第7d时,平均粒径由179nm增大到约280nm,且粒径随着时间的延长进一步增加.同时,添加组织蛋白酶B(C_B)的载药胶束的释药量及释药速率均高于未添加C_B的载药胶束.此外,利用人类胰腺癌细胞株(BxPC-3)对聚合物载药胶束、空白胶束和未经负载的游离DOX进行细胞毒性实验,结果表明C_(18)-VCPABC-mPEG胶束几乎没有细胞毒性,且载药胶束的毒性明显低于游离DOX.
An enzymatically degradable amphiphilic polymer, valine citrulline p-aminophenyl carbonate poly-B, was synthesized from the dipeptide valine citrulline (VC) (C18-VC-PABC-mPEG) .The polymer was self-assembled in water to form spherical micelles with uniform particle size distribution with an average diameter of about 179 nm.The enzyme degradation was studied by simulating lysosomal conditions Behavior and drug-loaded drug-resistant doxorubicin (DOX) micelles release behavior and found that the first 7d polymer micelles average particle size increased from 179nm to about 280nm, and the particle size as time goes on further While the release rate of drug-loaded micelles with cathepsin B (C_B) was higher than that of drug-loaded micelles without C-B addition.In addition, using the human pancreatic cancer cell line (BxPC-3) The results showed that C_ (18) -VCPABC-mPEG micelles had almost no cytotoxicity, and the drug-loaded micelles were significantly less toxic than the free drug-loaded micelles DOX.