期刊
MOLECULAR PHARMACEUTICS
卷 10, 期 6, 页码 2426-2434出版社
AMER CHEMICAL SOC
DOI: 10.1021/mp400039j
关键词
stearylamine; multidrug resistance; self-assembly; nanocarrier; teniposide; mitochondria
资金
- National Basic Research Program of China [2010CB934000, 2012CB932502, 2013CB932503, 2013CB932704]
- National Natural Science Foundation of China [30925041, 81270047]
- Shanghai Program [11 nm0505900]
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.
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