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Integrin α v β 3 -targeted liposomal drug delivery system for enhanced lung cancer therapy.

Authors :
Fu S
Zhao Y
Sun J
Yang T
Zhi D
Zhang E
Zhong F
Zhen Y
Zhang S
Zhang S
Source :
Colloids and surfaces. B, Biointerfaces [Colloids Surf B Biointerfaces] 2021 May; Vol. 201, pp. 111623. Date of Electronic Publication: 2021 Feb 13.
Publication Year :
2021

Abstract

Conventional chemotherapy for tumor treatment remains flawed because it fails to limit cytotoxicity to a small set of selectable tissues. Active targeting techniques for the delivery of drugs to specific sites are increasingly used to enhance drug accumulation at tumor sites with the aim of reducing side effects in vivo. Liposomes, modified with different targeting ligands, are considered to be one of the most promising targeted drug carriers. Herein, novel linear and cyclic arginine-glycine-aspartate (RGD) peptide-based lipids were synthesized to develop modified liposomal drug delivery systems with active targeting and pH-sensitivity. The RGD-modified liposomes showed excellent active targeting ability for integrin α <subscript>v</subscript> β <subscript>3</subscript> receptors, resulting in improved cellular uptake. The modified liposomes also enhanced intracellular doxorubicin (DOX) release because of their degradation in an acidic environment. Consequently, the RGD-modified, DOX-loaded liposomes exhibited significant antitumor efficacy and low toxicity in vitro and in vivo. In particular, 5% cRGD-lipid modified DOX-loaded liposome showed the greatest inhibition of tumor growth in mice among the tested formulations, and much less toxicity than free DOX. In conclusion, the DOX-loaded pH-sensitive liposome modified with 5% cRGD-lipid developed in the current study provides a potential approach for improved tumor therapy.<br /> (Copyright © 2021. Published by Elsevier B.V.)

Details

Language :
English
ISSN :
1873-4367
Volume :
201
Database :
MEDLINE
Journal :
Colloids and surfaces. B, Biointerfaces
Publication Type :
Academic Journal
Accession number :
33636597
Full Text :
https://doi.org/10.1016/j.colsurfb.2021.111623