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


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 of low molecular weight (ie, 2 kDa) methoxy poly(ethylene glycol) methyl ether (mPEG) to gambogic acid (GA-mPEG₂₀₀₀) through an ester linkage and characterized by (1)H nuclear magnetic resonance. The GA-mPEG₂₀₀₀ conjugates self-assembled to form nanosized micelles, with mean diameters of less than 50 nm, and a very narrow particle size distribution. The properties of the GA-mPEG₂₀₀₀ micelles, including morphology, stability, molecular modeling, and drug release profile, were evaluated. MTT (3-(4,5-dimethylthiazo l-2-yl)-2,5 diphenyl tetrazolium bromide) tests demonstrated that the GA-mPEG₂₀₀₀ micelle formulation had obvious cytotoxicity to tumor cells and human umbilical vein endothelial cells. Further, GA-mPEG₂₀₀₀ micelles were effective in inhibiting tumor growth and prolonged survival in subcutaneous B16-F10 and C26 tumor models. Our findings suggest that GA-mPEG₂₀₀₀ micelles may have promising applications in tumor therapy.

DOI: 10.2147/IJN.S54050

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@inproceedings{Cai2014ImprovingAS, title={Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles}, author={Lulu Cai and Neng Qiu and Mingli Xiang and Rongsheng Tong and Junfeng Yan and Lin He and Jianyou Shi and Tao Chen and Jiaolin Wen and Wenwen Wang and Lijuan Chen}, booktitle={International journal of nanomedicine}, year={2014} }