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Peptide modified liposomes with active recognizing of integrin αvβ3 for the treatment of melanoma

Published: 2016-11-16


Article from our customer: Kairong Shi, Journal of Controlled Release,2015.


Background: The use of pH-responsive cell-penetrating peptides (CPPs) is an attractive strategy for drug delivery in vivo, however, they still could not actively target to the desired sites. Here, we designed a pH-responsive CPP (TR) with the ability of active targeting to integrin αvβ3.


Results: TR-Lip could not only actively target to αvβ3-overexpressing cells compared to TH-Lip, but also significantly increased cellular uptake compared to RGD-Lip. At the concentration of 20 μg/mL paclitaxel (PTX), the killing activity of PTX-loaded TR-Lip (PTX-TR-Lip) against B16F10 cells was 1.80-, 1.45-, 1.30-, 1.15-time higher than that of PTX-loaded PEG-, RGD-, TH-modified liposomes and free PTX at pH 6.5, respectively. In vivo imaging displayed the maximum accumulation of DiD-labeled TR-Lip at tumor sites compared to the other groups. Tumor inhibition rate of B16F10 tumor-bearing mice treated with PTX-TR-Lip was 85.04%, relative to that of PBS. In B16F10 tumor-bearing mice, PTX-TR-Lip showed significantly higher survival rate compared with the other groups.


Conclusion: All the results in vitro and in vivo suggested that TR-Lip would be a potential delivery system for PTX to treat integrin αvβ3-overexpressing tumor-bearing mice.

Fig. 1. Schematic design of TR-Lip for integrin αvβ3-overexpressing tumor-targeted drug delivery. Tumor pH-induced TR-Lip for selective targeting to integrin αvβ3-overexpressing cells, improved cellular uptake, and enhanced tumor penetration.


In this article, TH peptide with a terminal cysteine (AGYLLGHINLHHLAHL(Aib)HHILCys), TR peptide with a terminal cysteine [c(RGDfK)-AGYLLGHINLHH LAHL(Aib)HHIL-Cys,lysine connected with alanine by covalent bonds]

were synthesized according to the standard solid phase peptide synthesis by ZheJiang Ontores Biotechnologies Co. Ltd. (Hangzhou, China).

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