摘要
目的制备Pluronic P105/PEG-PE/TPGS混合胶束系统,增加胶束被水冲稀后的稳定性,提高载药量。方法以普郎尼克P105(Pluronic P105)和聚乙二醇二乙酰基酯类的轭合物(PEG-PE)为材料采用薄膜水化法制备混合胶束系统,同时为增加胶束的载药量加入D-α-维生素E聚乙二醇1000琥珀酸酯(TPGS)。以难溶性抗癌药物喜树碱为模型药物,对混合胶束系统的载药量、冲稀后的稳定性进行了研究。采用人胸腺癌细胞系(MCF-7),对混合胶束的细胞毒性进行了研究。结果所制备的混合胶束系统,多倍冲稀后仍然能够稳定存在。同时与原料药相比极大增加难溶性药物的溶解度。细胞毒性结果表明,混合胶束的细胞毒性大大高于原料药。结论Pluronic P105/PEG-PE/TPGS混合胶束系统是一种潜在的抗癌药物给药系统。
Abstract
OBJECTIVE To increase the stability of poorly soluble anticancer drug camptothecin(CPT).METHODS Mixed micelles from the mixture of Pluronic P105,PEG-PE and D-α-tocopheryl polyethylene glycol 1000 succinate(TPGS) were prepared and loaded with the poorly soluble anticancer drug camptothecin(CPT).The drug loading and colloidal stability towards dilution were studied.The cytotoxicity of the CPT-loaded mixed micelles against MCF-7 cancer cell in vitro was determined. RESULTS The mixed micelles was stable after dilution.The solubilization of CPT by the mixed micelles was super to free drug. The cytotoxicity of the CPT-loaded mixed micelles against MCF-7 cancer cell in vitro was remarkably higher than that of the free drug.CONCLUSION Mixed micelles made of Pluronic/PEG-PE/TPGS is potential for drug delivery systems.
关键词
混合胶束 /
难溶药物 /
喜树碱 /
细胞毒性
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Key words
Pluronic mixed micelles /
poorly soluble anticancer drug /
camptothecin /
cytotoxicity
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杨兴国;李凌冰.
Pluronic P105/PEG-PE/TPGS混合胶束系统对喜树碱的增溶[J]. 中国药学杂志, 2009, 44(10): 762-765
YNG Xing-guo;LI Ling-ing.
Mixed Micelles Made of Pluronic/PEG-PE/TPGS for Solubilization of Camptothecin [J]. Chinese Pharmaceutical Journal, 2009, 44(10): 762-765
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脚注
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基金
山东省自然基金资助项目(Y2005C65)
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