基于低分子量甲基纤维素的温敏凝胶/泊洛沙姆胶束组合体系用于局部和持续递送多西他赛。
Low-molecular-weight methylcellulose-based thermo-reversible gel/pluronic micelle combination system for local and sustained docetaxel delivery.
机构信息
Department of Bioengineering, Institute for Bioengineering & Biopharmaceutical Research Hanyang University, 17, Haengdang-dong, Seongdong-gu, Seoul, 133-791, Republic of Korea.
出版信息
Pharm Res. 2012 Feb;29(2):525-34. doi: 10.1007/s11095-011-0581-8. Epub 2011 Sep 9.
PURPOSE
To develop low-molecular-weight methylcellulose (LMw MC)-based gel/Pluronic F127 micelle combination system for local and sustained delivery of docetaxel (DTX).
METHODS
LMw MC and Pluronic F127 were used to formulate an injectable thermo-reversible gel/micelle combination system containing DTX. The DTX-loaded combination system was characterized and its therapeutic efficacy evaluated in a subcutaneous tumor model.
RESULTS
Mixtures of LMw MC, AS, and Pluronic F127 formed gel at ~15-40°C depending on AS concentration. The combination system released DTX for >30 days with a biphasic and sustained release pattern, and DTX stability was maintained during release. The combination system significantly enhanced anti-cancer effects of DTX and prolonged survival of the model mouse in comparison with free DTX.
CONCLUSIONS
The LMw MC gel/Pluronic F127 micelle combination system constitutes a promising tool for reducing tumor size and eradicating remaining tumor cells before and after surgery.
目的
开发基于低分子量甲基纤维素（LMw MC）的凝胶/泊洛沙姆 F127 胶束组合系统，用于局部和持续递送达托泊替康（DTX）。
方法
采用 LMw MC 和泊洛沙姆 F127 来配制含有 DTX 的可注射温敏凝胶/胶束组合系统。对 DTX 载药组合系统进行了表征，并在皮下肿瘤模型中评估了其治疗效果。
结果
根据 AS 浓度的不同，LMw MC、AS 和泊洛沙姆 F127 的混合物在 15-40°C 之间形成凝胶。组合系统以双相和持续释放的方式释放 DTX 超过 30 天，并且在释放过程中保持 DTX 的稳定性。与游离 DTX 相比，该组合系统显著增强了 DTX 的抗癌作用，并延长了模型小鼠的存活时间。
结论
LMw MC 凝胶/泊洛沙姆 F127 胶束组合系统有望成为一种减少肿瘤体积和消除手术前后残留肿瘤细胞的工具。
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