PMID- 23679827
OWN - NLM
STAT- MEDLINE
DCOM- 20140115
LR  - 20130603
IS  - 1543-8392 (Electronic)
IS  - 1543-8384 (Linking)
VI  - 10
IP  - 6
DP  - 2013 Jun 3
TI  - Reversal of multidrug resistance by mitochondrial targeted self-assembled 
      nanocarrier based on stearylamine.
PG  - 2426-34
LID - 10.1021/mp400039j [doi]
AB  - 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.
FAU - Zhang, Zhiwen
AU  - Zhang Z
AD  - Center of Pharmaceutics, Shanghai Institute of Materia Medica, Chinese Academy of 
      Sciences, Shanghai 201203, China.
FAU - Liu, Zeying
AU  - Liu Z
FAU - Ma, Li
AU  - Ma L
FAU - Jiang, Shijun
AU  - Jiang S
FAU - Wang, Yixin
AU  - Wang Y
FAU - Yu, Haijun
AU  - Yu H
FAU - Yin, Qi
AU  - Yin Q
FAU - Cui, Jingbin
AU  - Cui J
FAU - Li, Yaping
AU  - Li Y
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20130516
PL  - United States
TA  - Mol Pharm
JT  - Molecular pharmaceutics
JID - 101197791
RN  - 0 (Amines)
RN  - 957E6438QA (Teniposide)
RN  - FFV58UNY7O (stearylamine)
SB  - IM
MH  - Amines/pharmacokinetics/*therapeutic use
MH  - Animals
MH  - Apoptosis/drug effects
MH  - Breast Neoplasms/*drug therapy
MH  - Cell Cycle/drug effects
MH  - Cell Proliferation/drug effects
MH  - Drug Resistance, Neoplasm/drug effects
MH  - Female
MH  - Humans
MH  - MCF-7 Cells
MH  - Membrane Potential, Mitochondrial/drug effects
MH  - Mice
MH  - Mice, Nude
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Teniposide/pharmacokinetics/therapeutic use
EDAT- 2013/05/18 06:00
MHDA- 2014/01/16 06:00
CRDT- 2013/05/18 06:00
PHST- 2013/05/18 06:00 [entrez]
PHST- 2013/05/18 06:00 [pubmed]
PHST- 2014/01/16 06:00 [medline]
AID - 10.1021/mp400039j [doi]
PST - ppublish
SO  - Mol Pharm. 2013 Jun 3;10(6):2426-34. doi: 10.1021/mp400039j. Epub 2013 May 16.