负载奥沙利铂纳米粒子的制备及抗肿瘤效果研究

Preparation and anti-tumor activity evaluation of oxaliplatin loaded nanoparticles

目的:采用聚乙二醇-聚乳酸羟基乙酸(mPEG-PLGA)二亲嵌段共聚物为载体,制备负载奥沙利铂的纳米粒子(nanoparticle,NP),全面考察其性质及体内抗肿瘤效果。方法:通过双乳化挥发法,制备奥沙利铂载药纳米粒子,考察纳米粒子的形态、粒径分布、稳定性、体外释放特性及体内抗肿瘤效果等性质。结果:所制得奥沙利铂纳米粒子为较规则的圆球形,平均粒径200.6-242.1nm,稳定性实验提示其稳定性良好;平均包封率和载药量分别为(65.62±1.27)%和(3.21±0.02)%,体外释放曲线显示了奥沙利铂纳米粒子良好的缓释特性。体内实验中,相比对照组和空白组,纳米粒子组能明显抑制肿瘤的生长,相对裸药组能明显降低药物的毒副反应,且能够延长小鼠的平均生存期。结论:实验结果为肿瘤"带瘤生存"的治疗理念提供了新的思路和科学依据。

Objective：Drug loaded nanoparticles are prepared by double emulsion - evaporatio method with mPEG - PLGA as drug carrier. Methods ： Oxaliplatin - loaded nanoparticles were prepared by double emulsion - evaporation method. The physical characteristics （size, stability and release pattern） and in vivo antitumor efficacy were evaluated to prove the advantage of drug loaded nanoparticles. Results：The size of oxaliplatin loaded nanopartieles was about 200.6 -242.1 nm. The drug loading content was （3.21 ± 0.02 ）% with the encapsulation efficiency reaching （65.62 ± 1.27 ） %. In vitro release study indicates the controlled release pattern of oxaliplatin - loaded nanoparticles. In vivo evaluation of oxaliplatin - loaded nanoparticles demonstrated enhanced antitumor effects and higher survival rate compared with the control group. Meanwhile, it can significantly reduce the side effects of the drug against free oxaliplatin. Conclusion：The effective drug- loaded nano- system conforms to ＂survival with tumor＂ ,the modern treatment concept.