Abstract：OBJECTIVE To embed imatinib(IMN) into micelles based on tocofersolan(TPGS) matrix , charecterize the physical and chemical properties of IMN-TPGS micelles and improve the anti-tumor effect. METHODS The thin film dispersion method was used to prepare IMN-TPGS micelles, and their particle size distribution, surface potential, morphology, drug loading, encapsulation efficiency and in vitro release behavior were characterized. The in vitro anti-tumor effect of IMN-TPGS micelles was investigated on MCF-7/ADR cells. RESULTS The average particle size of IMN-TPGS micelles was (22.69±2.39) nm, the drug loading was (1.55±0.06)%, and the encapsulation efficiency was (63.49±2.42)%. IMN-TPGS micelles with neutral surface showed a nearly sphere appearance. There was no significant change in diameter and drug loading after dilution times. IMN-TPGS micelles could be stable in the serum solution for 24 h. There was no significant difference in its particle size and encapsulation efficiency before and after freeze-drying. The in vitro cumulative release of IMN from TPGS micelles was close to 100% after 72 hours with a slow rate. The IC50 of the IMN-loaded TPGS micelles was 12.27μmol·L-1 consistent with its significant cellular uptake in MCF-7/ADR cells. CONCLUSION IMN-TPGS micelles with uniform particle size, good dispersibility and high stability, showed strong anti-dilution properties, which were conducive to the long circulation in body fluids. IMN-TPGS micelles exhibit obvious anti-tumor effects on drug-resistant cell lines, which could overcome multidrug resistance to a certain extent.
吕风梅, 李北雪, 周翔, 何駸頔, 随力, 刘哲鹏. 伊马替尼胶束的制备与体外克服肿瘤耐药性的研究[J]. 中国药学杂志, 2022, 57(7): 554-562.
LÜ Feng-mei, LI Bei-xue, ZHOU Xiang, HE Qin-di, SUI Li, LIU Zhe-peng. Preparation of Imatinib Micelles and Research on in Vitro Overcoming Tumor Drug Resistance. Chinese Pharmaceutical Journal, 2022, 57(7): 554-562.
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