Reversal of multidrug resistance by mitochondrial targeted self-assembled nanocarrier based on stearylamine.
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| Abstract |
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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| Authors | Zhiwen Zhang, Zeying Liu, Li Ma, Shijun Jiang, Yixin Wang, Haijun Yu, Qi Yin, Jingbin Cui, Yaping Li |
| Journal | Molecular pharmaceutics (Mol Pharm) Vol. 10 Issue 6 Pg. 2426-34 (Jun 03 2013) ISSN: 1543-8392 [Electronic] United States |
| PMID | 23679827 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't) |
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