6-Mercaptopurine/verapamil-mesoporous silica and reversing multidrug resistance

doi:10.3969/j.issn.1006-7795.2015.02.002

Journal of Capital Medical University ›› 2015, Vol. 36 ›› Issue (2): 161-165.doi: 10.3969/j.issn.1006-7795.2015.02.002

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6-Mercaptopurine/verapamil-mesoporous silica and reversing multidrug resistance

Xing Lu¹, Cui Chunying¹, Wang Yuji², Fang Chenjie¹, Wu Jianhui²

1. Department of Pharmacy, School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China;
2. Department of Medicinal Chemistry, School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China

Received:2014-12-08 Online:2015-04-21 Published:2015-04-16
Supported by:
This study was supported by Significant New Drugs Creation "Five-year" Plan Special Science and Technology Major(2011ZX09302-007-01).

Abstract

Abstract: Objective To prepare 6-mercaptopurine/verapamil-loaded mesoporous silica, to examine its in vitro antitumor activity and to evaluate if it can reverse drug-resistance. Methods The mesoporous silica nanoparticles(MSNS) were synthesized with copolycondensation method. Separately loaded 6-mercaptopurine and verapamil onto MSNS to construct 6-mercaptopurine/verapamil-mesoporous silica. Dynamic dialysis was used to analyze the in vitro drug release. The reversal of drug resistance of 6-mercaptopurine/verapamil-mesoporous silica was evaluated on MCF-7 and MCF-7/ADM cells using MTT assay. Results There are spherical microstructure, uniform distribution and regular mesoporous channels in the prepared carrier system with a grain diameter ranging from 170 nm to 250 nm and the Zeta potential was in the range of -30 mV to -40 mV. The in vitro drug release showed that no 6-mercaptopurine be released before the addition of DTT but 6-mercaptopurine was suddenly and then slowly released with the addition of DTT. The results of MTT assays showed that 6-mercaptopurine/verapamil-mesoporous silica carrier system had a good effect on the reversal of drug-resistance. Conclusion 6-mercaptopurine/verapamil-mesoporous silica carrier system has a good antitumor activity and can reverse drug resistance.

Key words: mesoporous silica nanoparticles, 6-mercaptopurine, multidrug resistance(MDR), antitumor

CLC Number:

Xing Lu, Cui Chunying, Wang Yuji, Fang Chenjie, Wu Jianhui. 6-Mercaptopurine/verapamil-mesoporous silica and reversing multidrug resistance[J]. Journal of Capital Medical University, 2015, 36(2): 161-165.

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6-Mercaptopurine/verapamil-mesoporous silica and reversing multidrug resistance

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