目的 考察以两亲嵌段共聚物mPEG - PCL所制备的多西紫杉醇(Doc)载药纳米粒子的靶向抗肿瘤作用,并对其机理进行探讨.方法 采用丙酮-纳米沉淀法制备负载Doc的纳米粒子,动态光散射测定纳米粒子载药前后的粒径及多分散性.采用荧光标记粒子细胞摄取实验,探讨Doe纳米粒子抗肿瘤作用不同于裸药的机制.建立小鼠肝癌细胞H22皮下移植瘤模型,研究尾静脉注射载药纳米粒子的体内抗肿瘤作用.结果 通过纳米沉淀法制备的空白粒子平均粒径为75.7 nm,多西紫杉醇载药粒子的平均粒径为78.0 nm.体内实验结果显示单次尾静脉给药,多西紫杉醇纳米粒子的抗肿瘤效果明显优于临床上常用的泰素帝(P＜0.01).结论 高分子多西紫杉醇载药纳米粒子可以提高多西紫杉醇的体内抗肿瘤效果,显示出良好的临床应用前景.%Objective To study the curative effects and possible mechanism of docetaxel (Doc) - loaded nanoparticles with bi - block copolymers mPEG - PCL against hepatic carcinoma. Methods mPEG - PCL was synthesized by ring - opening polymerization method and the nanodrug was prepared by acetone nano - precipated method. The diameters and polydispersity of the nanoparticles were evaluated by dynamic light scattering ( DLS). The in vivo antitumor effect of Doc - loaded nanoparticles was investigated on hepatic H22 tumor model via intravenous administration. Results The diameters of blank nanoparticles and Doc - loaded nanoparticle were 75. 5 and 78. 0 nm respectively. Vivo and - tumor effect showed the tumor growth inhibition of Doc - loaded nanoparticles was markedly smaller than commercial taxotere (P < 0. 01). Conclusion DOC - loaded nanoparticles could enhance the antitumor effect of taxotere and has potential for future clinical application.
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