紫杉醇mPEG-PLGA纳米粒的制备及其抗肿瘤作用研究

 目的探讨负载紫杉醇的聚乙二醇单甲醚-聚乳酸-乙醇酸(mPEG-PLGA)亲性嵌段共聚物纳米粒及其对肝癌H22细胞的体内抗肿瘤作用。方法采用界面沉积法制备紫杉醇mPEG-PLGA纳米粒(Ptx-Nps);应用透射电镜表征纳米粒的形态;粒径分析仪测其粒径及Zeta电位;研究mPEG在共聚物中的含量及紫杉醇投药量对纳米粒的影响;考察纳米粒对昆明小鼠肝癌H22的疗效和过敏实验。结果Ptx-Nps成球型,粒径为纳米级(<120 nm),均带负电荷(适合于静脉注射),与紫杉醇注射液(Ptx)相比,Ptx-Nps对肝癌H22的抑制作用比Ptx好。结论采用界面沉积法制备的纳米粒在紫杉醇投药量为1%,mPEG含量为4%时包封率最佳,本研究为开发紫杉醇新型静脉注射制剂提供了实验依据,mPEG-PLGA共聚物可成为抗肿瘤药物的理想新型载体。

Studis on Preparation of Paclitaxel-loaded mPEG-PLGA Nanoparticles and Its Inhibition Effect on Tumor

OBJECTIVE To investigate the characterization of paclitaxel-loaded methoxy poly(ethylene glyeol)-poly(lactic-co-glycolic acid) copolymer nanoparticles and the anti-tumoral activity of the Ptx-Nps on mice liver cancer H22.METHODS The paclitaxel(Ptx) poly(ethylene glyeol-lactic-co-glycolic acid)(mPEG-PLGA) nanoparticles were prepared by the interfacial deposition method.The particle size and Zeta potential were evaluated by Malvern Zertasizer.The morphology of mPEG-PLGA Ptx/Nps was characterized by transmission electron microscopy.The influences of the paclitaxel-fed amount and different contents of mPEG in the copolymer on Ptx-Nps were studied.Therapeutic effect of the Nps was studied on Kunming mice liver cancer H22 and hypersusceptible test was also carried out.RESULTS Ptx-Nps of preparation allowed the formation of spherical nanometric(<120 nm),homogeneous and negatively charged particles which were suitable for intravenous administration.The tumor inhibiting effect of Ptx-Nps was more effective compared with paclitaxel injection.CONCLUSION The incorporation efficiency of paclitaxel in nanoparticles was the best when using 1% paclitaxel-fed amount and 4% mPEG in the copolymer.This study will provide an experiment basis for the development of new kind of intravenous administration of paclitaxel,mPEG-PLGA copolymer becomes a new perfect material of anti-tumoral drug.