College of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.
Drug Deliv. 2011 Apr;18(3):181-9. doi: 10.3109/10717544.2010.520355. Epub 2010 Oct 13.
A water-insoluble anti-tumor agent, Paclitaxel (PTX) was successfully incorporated into polymeric micelles formed from new graft copolymers, N-octyl-N-(2-carboxyl-cyclohexamethenyl) chitosan derivatives(OCCC). The objective of this study was to optimize and characterize the novel PTX micelle (PTX-M). Furthermore, the pharmacokinetics, NIR-imaging, biodistribution, and anti-tumor effects of PTX-M were evaluated. The results showed that the PTX-M had high drug loading (43.25%). The Vd and t1/2β of PTX-M were increased by 11.4- and 2.83-fold, respectively, but the plasma AUC of PTX-M was 3.8-fold lower than that of Taxol. Biodistribution study indicated that PTX-M was widely distributed into most tissues, most of them found in liver, spleen, lung, and kidney. This result was similar with NIR(near-infrared)-imaging. Tumor growth was significantly inhibited after intravenous injection of PTX-M. PTX-M showed the enhanced anti-tumor effect and non-toxic effects compared with Taxol, the commercial product of PTX. Therefore, the chitosan-derived micelle system offered a stable and effective platform for cancer chemotherapy with PTX.
一种水溶性抗肿瘤药物紫杉醇（PTX）成功地掺入了由新型接枝共聚物 N-辛基-N-（2-羧基环己亚甲基）壳聚糖衍生物（OCCC）形成的聚合物胶束中。本研究的目的是优化和表征新型 PTX 胶束（PTX-M）。此外，还评估了 PTX-M 的药代动力学、近红外成像、生物分布和抗肿瘤作用。结果表明，PTX-M 的载药量较高（43.25%）。PTX-M 的 Vd 和 t1/2β 分别增加了 11.4 倍和 2.83 倍，但 PTX-M 的血浆 AUC 却降低了 3.8 倍。生物分布研究表明，PTX-M 广泛分布于大多数组织中，大部分分布在肝脏、脾脏、肺和肾脏中。这一结果与近红外（NIR）成像相似。静脉注射 PTX-M 后，肿瘤生长明显受到抑制。与紫杉醇（PTX）的商业产品 Taxol 相比，PTX-M 显示出增强的抗肿瘤作用和低毒性作用。因此，壳聚糖衍生的胶束系统为 PTX 的癌症化疗提供了一个稳定有效的平台。
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