Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles

• DOI: 10.2147/ijn.s54050
• Publication Date: 2013-12-29T20:46:25Z
• Authors: lijuan Chen; Lulu Cai; Neng Qiu; Mingli Xiang; Rongsheng Tong; Junfeng Yan; Lin He; Jianyou Shi; Tao Chen; Jiaolin Wen; Wenwen Wang
• Keywords: Gambogic acid

The clinical application of gambogic acid, a natural component with promising antitumor activity, is limited due to its extremely poor aqueous solubility, short half-life in blood, and severe systemic toxicity. To solve these problems, an amphiphilic polymer-drug conjugate was prepared by attachment low molecular weight (ie, 2 kDa) methoxy poly(ethylene glycol) methyl ether (mPEG) acid (GA-mPEG₂₀₀₀) through ester linkage characterized (1)H nuclear magnetic resonance. GA-mPEG₂₀₀₀ conjugates self-assembled form nanosized micelles, mean diameters less than 50 nm, very narrow particle size distribution. properties the including morphology, stability, modeling, drug release profile, were evaluated. MTT (3-(4,5-dimethylthiazo l-2-yl)-2,5 diphenyl tetrazolium bromide) tests demonstrated that micelle formulation had obvious cytotoxicity tumor cells human umbilical vein endothelial cells. Further, micelles effective inhibiting growth prolonged survival subcutaneous B16-F10 C26 models. Our findings suggest may have applications therapy.