National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
J Control Release. 2011 May 30;152(1):49-56. doi: 10.1016/j.jconrel.2011.02.031. Epub 2011 Mar 22.
pH-sensitive poly(ethylene glycol)-poly(L-histidine)-poly(L-lactide) (PEG-PH-PLLA) nanoparticles were prepared and used as carriers for anti-tumor drug delivery. The morphology and properties of the nanoparticles such as pH sensitivity, zeta potential and mean diameters were investigated. The cytotoxicity of PEG-PH-PLLA nanoparticles was evaluated. Doxorubicin (DOX) was encapsulated in the nanoparticles to explore the release profile. The drug-loaded nanoparticles were incubated with HepG2 cells to study the in vitro anti-tumor effect. The results showed the sizes of both blank nanoparticles and drug-loaded nanoparticles in pH 7.4 were smaller than those of nanoparticles in pH 5.0, and the mean diameter of drug-loaded nanoparticles was much bigger than that of blank nanoparticles. The PEG-PH-PLLA nanoparticles were nontoxic to both NIH 3T3 fibroblasts and HepG2 cells. The release profile showed that the release of DOX in pH 5.0 was much faster than that in pH 7.4. The in vitro experiments demonstrated that the anti-tumor effect of drug-loaded nanoparticles was preferable to free doxorubicin. The pH-sensitive PEG-PH-PLLA nanoparticles are promising carriers for anti-tumor drug delivery.
pH 敏感型聚乙二醇-聚组氨酸-聚乳酸（PEG-PH-PLLA）纳米粒被制备并用作抗肿瘤药物载体。研究了纳米粒的形态和性能，如 pH 敏感性、Zeta 电位和平均粒径。评价了 PEG-PH-PLLA 纳米粒的细胞毒性。阿霉素（DOX）被包封在纳米粒中以探索释放特性。载药纳米粒与 HepG2 细胞孵育以研究体外抗肿瘤作用。结果表明，在 pH 7.4 时空白纳米粒和载药纳米粒的粒径均小于 pH 5.0 时的粒径，且载药纳米粒的平均粒径明显大于空白纳米粒。PEG-PH-PLLA 纳米粒对 NIH 3T3 成纤维细胞和 HepG2 细胞均无毒性。释放特性表明，在 pH 5.0 时 DOX 的释放速度明显快于 pH 7.4。体外实验表明，载药纳米粒的抗肿瘤效果优于游离阿霉素。pH 敏感型 PEG-PH-PLLA 纳米粒是一种有前途的抗肿瘤药物载体。
