长春碱纳米粒的制备及其抗肿瘤活性

Preparation of Vinblastine Nanoparticles and Its Anti-tumor Effect

以右旋糖苷为稳定剂,通过乳化聚合法制备长春碱聚氰基丙烯酸正丁酯纳米粒,检测其基本性质(形态、粒径分布、包封率和载药量)。通过MTT法检测长春碱纳米粒对神经胶质瘤细胞BT325的细胞毒性作用、经倒置显微镜观察和HE染色,探讨了长春碱纳米粒对神经胶质瘤细胞BT325形态的影响。结果显示,长春碱纳米粒平均粒径为74.4nm,包封率为78.47%,载药量为39.24%。与长春碱原料药组相比,长春碱纳米粒组细胞吸光度显著降低,细胞数量明显减少,凋亡细胞增多。聚氰基丙烯酸丁酯纳米粒可作为长春碱进入胶质瘤细胞的有效载体。

Vinblastine loaded poly（butyl cyanoacrylate） nanoparticles（VLB-PBCA-NP） were prepared, by emulsion polymerization process and using dextran as a stabilizing agent. Vinblastine nanoparticles were characterized, by means of morphology, size, drug entrapment efficiency and loading efficiency. VLB-PBCA-NP cytotoxicity profile was monitored using BT325 glioma cells by MTT assay. Morphological character was observed by inverted microscope and HE staining. The results showed that mean diameter of VLB- PBCA-NP was about 74.4 nm, and drug entrapment efficiency and loading efficiency was 78.47% and 39.24%, respectively. Entrapment of vinblastine in nanoparticles may distinctly degrade absorbency and induce the amount of cells loss and apoptosis as compared to free drugs. PBCA may be effective as promising carrier for the transport of vinblastine into the glioma cells.