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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 based on a boronic ester bond was prepared for the treatment of prostate cancer. The nanoparticles can be self-assembled in aqueous solution to form nanoparticles. Transmission electron microscopy showed that the average particle size was 40 nm and could be uniformly dispersed. In vitro drug release experiments show that it has a pH-responsive drug release behavior. In vitro cytotoxicity results showed that its half-value inhibitory concentration (IC50) on prostate cancer cells is lower than that of normal cells, showing therapeutic targeting. The nanoparticles have some potential applications in the target transfer of gossypol and the treatment of prostate cancer.