pH响应型透明质酸-棉酚纳米粒子的制备及其性能研究

Preparation and Characteristics Study of the pH-Responsive Hyaluronic Acid-Gossypol Nanoparticles

制备了基于硼酸酯键的pH响应型透明质酸-棉酚缀合物,用于治疗前列腺癌。其在水溶液中可自组装形成纳米粒子,透射电镜观测表明其平均粒径40 nm,可均匀分散。体外药物释放实验证明,其具有pH响应的释药行为。体外细胞毒性结果显示其对前列腺癌细胞的半数抑制浓度(IC50)较正常细胞低,表现出治疗靶向性。该纳米粒子在棉酚的靶向传递及前列腺癌治疗方面具有一定的应用潜力。

A pH-responsive hyaluronic acid-gossypol conjugate was prepared based on boronate ester,which could be used as prostate cancer therapy. The conjugate could self-assemble into nanoparticle which morphology was observed by transmission electron microscopy. The nanoparticles were well-dispersed with 40 rnn diameter. The pH responsible drug release behavior was confirmed by in vitro drug release study. In vitro cytotoxicity study illustrated a favorable selectivity,since the half maximal inhibitory concentration （IC50） of the nanopaticles against prostate cancer cells was lower than that of normal cells.The designed nanoparticle showed great potential for targeted delivery of gossypol and treatment of prostate cancer.