Department of Oncology, First Affiliated Hospital of Nanjing Medical University, Nanjing, PR China.
Oncol Res. 2013;20(7):265-74. doi: 10.3727/096504012x13522227232318.
Successful chemotherapy needs to reduce the toxic side effects against normal tissues and avoid the detriments caused by intolerable solvents. Drug delivery systems using soluble polymeric nanoparticles tend to be the focus. In the current study, core-shell structure nanoparticles were prepared from block copolymer of methoxy poly(ethylene glycol)-polycaprolactone (mPE-PCL). Paclitaxel (PTX) and berbamine (BA) were incorporated into mPEG-PCL nanoparticles. It was found in our study that PTX and BA can be incorporated into the nanoparticles with high encapsulation efficiency. In vitro release study showed that PTX and BA were released from nanoparticles in a sustained manner. In vitro cytotoxicity studies indicated that PTX/BA coloaded nanoparticles (PTX/BA-np) show dose- and time-dependent cytotoxicity again BGC823 cells. Furthermore, intratumoral administration was applied to improve the tumor-targeted delivery in the in vivo evaluation. Compared with free drugs, PTX/BA-np exhibited superior antitumor effect by delaying tumor growth when delivered intratumorally. These results suggest that PTX/BA-np are effective to inhibit the growth of human gastric cancer and merit more research to evaluate the feasibility of clinical application.
成功的化疗需要降低对正常组织的毒性副作用，并避免因不可耐受的溶剂而造成的损害。使用可溶性聚合物纳米粒子的药物传递系统往往是研究的重点。在本研究中，从甲氧基聚（乙二醇）-聚己内酯（mPE-PCL）嵌段共聚物制备了核壳结构纳米粒子。紫杉醇（PTX）和小檗胺（BA）被包封在 mPEG-PCL 纳米粒子中。研究发现，PTX 和 BA 可以以高包封效率被包封入纳米粒子中。体外释放研究表明，PTX 和 BA 可以从纳米粒子中以持续的方式释放。体外细胞毒性研究表明，PTX/BA 共载纳米粒子（PTX/BA-np）对 BGC823 细胞表现出剂量和时间依赖性的细胞毒性。此外，还进行了瘤内给药以在体内评价中改善肿瘤靶向递送。与游离药物相比，PTX/BA-np 通过瘤内给药延迟肿瘤生长表现出更好的抗肿瘤效果。这些结果表明，PTX/BA-np 可有效抑制人胃癌的生长，值得进一步研究以评估其临床应用的可行性。
