文献类型：期刊文献

英文题名：Reversal of Multidrug Resistance by Mitochondrial Targeted Self-Assembled Nanocarrier Based on Stearylamine

作者：Zhang, Zhiwen[1];Liu, Zeying[2];Ma, Li[1];Jiang, Shijun[2];Wang, Yixin[1];Yu, Haijun[1];Yin, Qi[1];Cui, Jingbin[2];Li, Yaping[1]

机构：[1]Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Pharmaceut, Shanghai 201203, Peoples R China;[2]E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

年份：2013

卷号：10

期号：6

起止页码：2426

外文期刊名：MOLECULAR PHARMACEUTICS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000320015600033)】；

基金：The National Basic Research Program of China (2010CB934000, 2012CB932502, 2013CB932503, and 2013CB932704), the National Natural Science Foundation of China (30925041, 81270047), and Shanghai Program (11 nm0505900) are gratefully acknowledged for financial support.

语种：英文

外文关键词：stearylamine; multidrug resistance; self-assembly; nanocarrier; teniposide; mitochondria

摘要：Multidrug resistance (MDR) remains one of the major challenges for successful chemotherapy. Herein, we tried to develope a mitochondria targeted teniposide loaded self assembled nanocarrier based on stearylamine (SA-TSN) to reverse MDR of breast cancer. SA-TSN was nanometer-sized spherical particles (31.59 +/- 3.43 nm) with a high, encapsulation efficiency (99.25 +/- 0.21%). The MDR in MCF-7/ADR cells was obviously reduced by SA-TSN, which mainly attributed to the markedly reduced expression of P-gp, increased percentages in G2 phase, selectively accumulation in mitochondria, decrease of mitochondrial membrane potential, and greatly improved apoptosis. The plasma concentration of teniposide was greatly improved by SA-TSN, and the intravenously administered SA-TSN could accumulate in the tumor site and penetrate into the inner site of tumor in MCF-7/ADR induced xenografts. In particular, the in vivo tumor inhibitory efficacy of SA-TSN in MCF-7/ADR induced models was more effective than that of teniposide loaded self-assembled nanocarrier without stearylamine (TSN) and teniposide solution (TS), which verified the effectiveness of SA-TSN in reversal of MDR. Thereby, SA-TSN has potential to circumvent the MDR for the chemotherapy of breast cancer.