Shim Woo Sun, Kim Jong-Ho, Kim Kwangmeyung, Kim Yoo-Shin, Park Rang-Woon, Kim In-San, Kwon Ick Chan, Lee Doo Sung
Department of Polymer Science & Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
Int J Pharm. 2007 Feb 22;331(1):11-8. doi: 10.1016/j.ijpharm.2006.09.027. Epub 2006 Sep 23.
Paclitaxel (PTX) was loaded into synthetic pH/T-sensitive block copolymer (OSM-PCLA-PEG-PCLA-OSM) solution with various concentrations. The phase diagram of PTX-loaded block copolymer solution shifted to lower temperature region compared to net block copolymer because of the salting-out effect of PTX. Release profiles of PTX showed sustained manner regardless of loading amount of PTX. To evaluate anti-tumor effect of PTX-loaded block copolymer, solutions were injected subcutaneously to tumor-bearing mice and TUNEL assay examined. PTX-loaded block copolymer hydrogel for in vivo use showed good anti-tumor effect for 2 weeks and induced strong apoptosis in tumor tissue. Therefore, we conclude OSM-PCLA-PEG-PCLA-OSM block copolymer as an effective injectable carrier of PTX.
将紫杉醇(PTX)装载到具有不同浓度的合成pH/温度敏感嵌段共聚物(OSM-PCLA-PEG-PCLA-OSM)溶液中。由于PTX的盐析效应,与纯嵌段共聚物相比,载PTX嵌段共聚物溶液的相图向较低温度区域移动。PTX的释放曲线显示出持续释放的方式,与PTX的装载量无关。为了评估载PTX嵌段共聚物的抗肿瘤效果,将溶液皮下注射到荷瘤小鼠体内,并进行TUNEL检测。用于体内的载PTX嵌段共聚物水凝胶在2周内显示出良好的抗肿瘤效果,并在肿瘤组织中诱导强烈的细胞凋亡。因此,我们得出结论,OSM-PCLA-PEG-PCLA-OSM嵌段共聚物是一种有效的PTX可注射载体。