Jeong Young-Il, Na Hee-Sam, Cho Kyoung-Oh, Lee Hyun-Chul, Nah Jae-Woon, Cho Chong-Su
Department of Polymer Science and Engineering, Sunchon National University, Jeonnam 540-742, Republic of Korea.
Int J Pharm. 2009 Jan 5;365(1-2):150-6. doi: 10.1016/j.ijpharm.2008.08.011. Epub 2008 Aug 22.
The multiblock copolymer composed of poly(gamma-benzyl L-glutamate) (PBLG) and poly(ethylene oxide) (PEO) was synthesized to prepare polymeric micelles as an anticancer drug carrier. Adriamycin (ADR) used as an anticancer drug was incorporated into the polymeric micelles prepared by the multiblock copolymer. The higher the drug feeding ratio, the higher the drug loading contents and the lower the drug loading efficiency. The increased drug feeding ratio resulted in increased particle sizes. At all of the formulations, particle sizes were less than 150 nm. The particles were observed as spherical shapes. ADR release from ADR-loaded polymeric micelles in vitro was decreased with an increased drug loading contents. In in vitro antitumor activity test using CT 26 tumor cells, polymeric micelles showed almost similar cytotoxicity when compared to ADR itself while polymeric micelles themselves did not affect cytotoxicity. In in vivo antitumor activity test using mice tumor xenograft model, the polymeric micelles showed improved survivability of mice with minimized weight changes and excellent tumor growth suppression efficacy. Polymeric micelles of the multiblock copolymer suggested to be a good candidate for anticancer drug delivery carrier.
合成了由聚(γ-苄基-L-谷氨酸)(PBLG)和聚环氧乙烷(PEO)组成的多嵌段共聚物,以制备聚合物胶束作为抗癌药物载体。将用作抗癌药物的阿霉素(ADR)掺入由多嵌段共聚物制备的聚合物胶束中。药物投料比越高,载药量越高,载药效率越低。药物投料比的增加导致粒径增大。在所有制剂中,粒径均小于150nm。观察到颗粒为球形。载药聚合物胶束在体外的阿霉素释放随载药量的增加而降低。在使用CT 26肿瘤细胞的体外抗肿瘤活性试验中,与阿霉素本身相比,聚合物胶束表现出几乎相似的细胞毒性,而聚合物胶束本身不影响细胞毒性。在使用小鼠肿瘤异种移植模型的体内抗肿瘤活性试验中,聚合物胶束显示出小鼠存活率提高,体重变化最小,肿瘤生长抑制效果优异。多嵌段共聚物的聚合物胶束被认为是抗癌药物递送载体的良好候选者。