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Cyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery

Authors Lim C, Moon J, Sim T, Hoang NH, Won WR, Lee ES, Youn YS, Choi HG, Oh K, Oh KT

Received 20 April 2018

Accepted for publication 8 June 2018

Published 10 August 2018 Volume 2018:13 Pages 4627—4639

DOI https://doi.org/10.2147/IJN.S171794

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Thiruganesh Ramasamy

Peer reviewer comments 2

Editor who approved publication: Dr Thomas Webster


Chaemin Lim,1,* Junseong Moon,1,* Taehoon Sim,1 Ngoc Ha Hoang,1 Woong Roeck Won,1 Eun Seong Lee,2 Yu Seok Youn,3 Han-Gon Choi,4 Kyungsoo Oh,1 Kyung Taek Oh1

1College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea; 2Division of Biotechnology, The Catholic University of Korea, Bucheon, Republic of Korea; 3School of Pharmacy, SungKyunKwan University, Suwon, Republic of Korea; 4College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Republic of Korea

*These authors contributed equally to this work

Background: Blending micellar systems of different types of polymers has been proposed as an efficient approach for tailor-made drug formulations. The lamellar structure of hydrophobic polymers may provide a high drug loading capacity, and hydrophilic polymers may provide good colloidal stability.
Methods: In this study, the anticancer model drug docetaxel was loaded onto a nanosized blending micellar system with two pluronics (L121/F127). To achieve increased antitumor activity, the cyclic arginine-glycine-aspartic acid tripeptide (cRGD) as an active tumor targeting ligand was conjugated to the blending system.
Results: The docetaxel-loaded Pluronic blending system exhibited a higher drug loading capacity than that of F127 and showed high colloidal stability with a spherical structure. cRGD conjugates demonstrated enhanced drug cellular uptake and anticancer activity against αvβ3 integrin-overexpressing U87MG cancer cells. In vivo animal imaging also revealed that the prepared cRGD-conjugated nanoparticles effectively accumulated at the targeted tumor site through an active and passive targeting strategy.
Conclusion: Accordingly, the prepared nanosized system shows potential as a tailor-made, active targeting, nanomedicinal platform for anticancer therapy. We believe that this novel nanoplatform will provide insights for advancement of tumor therapy.

Keywords: blending micellar system, docetaxel, cyclic RGD, Pluronic L121/F127, active targeting, nanomedicine

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