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Folate-conjugated and pH-responsive polymeric micelles for target-cell-specific anticancer drug delivery.
- 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.)
- Subjects :
- A549 Cells
Animals
Citric Acid chemistry
Delayed-Action Preparations chemistry
Delayed-Action Preparations pharmacokinetics
Delayed-Action Preparations pharmacology
HeLa Cells
Hep G2 Cells
Humans
Hydrogen-Ion Concentration
Male
Mice
Mice, Inbred BALB C
Mice, Nude
Neoplasms, Experimental metabolism
Neoplasms, Experimental pathology
Polylactic Acid-Polyglycolic Acid Copolymer
Xenograft Model Antitumor Assays
Doxorubicin chemistry
Doxorubicin pharmacokinetics
Doxorubicin pharmacology
Lactic Acid chemistry
Lactic Acid pharmacokinetics
Lactic Acid pharmacology
Micelles
Neoplasms, Experimental drug therapy
Polyglycolic Acid chemistry
Polyglycolic Acid pharmacokinetics
Polyglycolic Acid pharmacology
Subjects
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