A comprehensive study of iRGD-modified liposomes with improved chemotherapeutic efficacy on B16 melanoma

Abstract

(2015) A comprehensive study of iRGD-modified liposomes with improved chemotherapeutic efficacy on B16 melanoma, Drug Delivery, 22:1, 10-20, DOI: 10.3109/10717544.2014 Here, iRGD-modified and doxorubicin-loaded sterically stabilized liposomes (iRGD-SSL-DOX) and passive liposomes (SSL-DOX) were prepared. A series of experiments were performed to evaluate the tissue penetration, cell penetration, tumor blood vessel damage and anti-tumor effect. The results of flow cytometry and confocal microscopy studies showed that iRGD-SSL-DOX with 5% DSPE-PEG 2000 -iRGD achieved higher cellular uptake level than that of SSL-DOX on B16 melanoma cells. iRGD-SSL-DOX also exhibited stronger cell growth inhibition in cytotoxicity experiments. The tumor penetrating effect of iRGD was further confirmed by imaging and cellular uptake studies in vivo, in which higher distribution of iRGD-modified liposomes in tumor tissue and tumor cells was observed. Moreover, iRGD-SSL-DOX displayed improved tumor growth inhibition and anti-angiogenesis with less systemic toxicity in an armpit B16 melanoma model. In conclusion, iRGD reserved its tumor-penetrating properties well when modified on the surface of liposomes at optimal density and iRGD-SSL-DOX would be a promising drug delivery system for active targeting tumor therapy.

Model Affitin and PEG modifications onto siRNA lipid nanocapsules: cell uptake and in vivo biodistribution improvements

“…12 The graing of Affitins on the LNC surface, a small articial model binding protein, modied the behavior of LNCs as already observed for nanomedicines modied with peptides. 41,44 As a rst step toward active targeting with LNCs, we wanted to study if an Affitin model, i.e. without any affinity for a melanoma biomarker, had intrinsic properties compatible with our goals.…”

A Novel Strategy to Improve the Therapeutic Efficacy of Gemcitabine for Non-Small Cell Lung Cancer by the Tumor-Penetrating Peptide iRGD

“…first reported the C-end rule peptide (iRGD), and demonstrated that the peptide possesses the activity of NRP-1-dependent cell, vascular, and tissue penetration [32]. Subsequent reports showed that iRGD could enhance the intratumoral dissemination and antitumor efficacy of Doxorubicin [33–35], Paclitaxel [36, 37] and Endostatin [38] by conjugating with these drugs or drug-loaded vehicles in animal experiments. The other reports demonstrated that iRGD also could enhance the intratumoral accumulation and antitumor efficacy of Paclitaxel, Doxorubicin, Transtuzumab [24, 39], Cisplatin [40], by co-administration with these drugs.…”

Targeted delivery of etoposide to cancer cells by folate-modified nanostructured lipid drug delivery system

“…The tumor inhibition efficiency of FA-ETPNLCs, ETP-NLCs and was 88%, 77% and 38%, respectively. Better tumor inhibition efficiency indicates that FA-ETPNLCs showed better antitumor activity than ETP-NLCs and ETP solution for the treatment of gastric cancer in vivo (Dai et al, 2015). Obviously, decreased body weights, reduced foods intake and inactive moving behavior were found in ETP solution, blank NLCs and saline control groups.…”