Back to Search Start Over

Folate-conjugated and pH-responsive polymeric micelles for target-cell-specific anticancer drug delivery.

Authors :
Guan J
Zhou ZQ
Chen MH
Li HY
Tong DN
Yang J
Yao J
Zhang ZY
Source :
Acta biomaterialia [Acta Biomater] 2017 Sep 15; Vol. 60, pp. 244-255. Date of Electronic Publication: 2017 Jul 14.
Publication Year :
2017

Abstract

In this study, we developed a folate (FA)-conjugated and pH-responsive active targeting micellar system for anti-cancer drug delivery. In this system, FA was attached to the terminal of the hydrophilic segment of poly(lactic acid)-poly(L-lysine) (PLA-PLL), and PLL was modified by a citric acid group. The FA receptor-mediated active targeting and electrostatic interaction between micelles and cell membrane due to a negative-to-positive charge reversal was combined in one micellar anti-cancer drug delivery system to enhance the tumour targeting and cellular internalisation of micelles. In vitro and in vivo anti-cancer studies demonstrated that the doxorubicin-loaded, FA-conjugated and pH-responsive polymeric micelles possess an enhanced and effective cancer efficiency.<br />Statement of Significance: Negatively charged nano-carriers prolonged anti-cancer drugs' blood circulation. However it is difficult to be internalised. Therefore, a negative-to-positive charged micelle surface could improve selectivity for tumour cells and increase uptake chance. In this study, we developed a folate (FA)-conjugated and pH-responsive active targeting micellar system for anti-cancer drug delivery. The FA receptor-mediated active targeting and electrostatic interaction between micelles and cell membrane due to a negative-to-positive charge reversal was combined in one micellar anti-cancer drug delivery system to enhance the tumour targeting and cellular internalisation of micelles. In vitro and in vivo anti-cancer studies demonstrated that the doxorubicin-loaded, FA-conjugated and pH-responsive polymeric micelles possess an enhanced and effective cancer efficiency.<br /> (Copyright © 2017. Published by Elsevier Ltd.)

Details

Language :
English
ISSN :
1878-7568
Volume :
60
Database :
MEDLINE
Journal :
Acta biomaterialia
Publication Type :
Academic Journal
Accession number :
28713015
Full Text :
https://doi.org/10.1016/j.actbio.2017.07.018