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Open AccessArticle

Anticancer Effect of Metformin in Herceptin-Conjugated Liposome for Breast Cancer

by Ji-Yeon Lee 1,†, Dae Hwan Shin 2 and Jin-Seok Kim 1,*
1
Drug Information Research Institute (DIRI), College of Pharmacy, Sookmyung Women’s University, Cheongparo 47 gil 100, Yongsan gu, Seoul 04310, Korea
2
College of Pharmacy, Chungbuk National University, Cheongju 28160, Korea
*
Author to whom correspondence should be addressed.
Present address: Kolon Pharma R&D Center, 45 18-gil, Munpyeongseo-ro, Daedeog-gu, Daejeon 34302, Korea.
Pharmaceutics 2020, 12(1), 11; https://doi.org/10.3390/pharmaceutics12010011
Received: 22 October 2019 / Revised: 27 November 2019 / Accepted: 18 December 2019 / Published: 20 December 2019
(This article belongs to the Special Issue Advances in Liposome-Based Drug Delivery Systems)
Metformin (MET) is an anti-diabetic drug effective against breast cancer, targeting breast cancer stem cells (BCSCs). MET-encapsulating liposome (LP-MET) and Herceptin-conjugated LP-MET (Her-LP-MET) were evaluated for their anti-cancer effect in vitro and in vivo. Size and zeta potentials of LP-MET and Her-LP-MET were suitable for enhanced permeability and retention effects. Her-LP-MET yielded greater inhibition of BCSC proliferation in vitro than free MET or LP-MET, as well as a dose-dependent long-term anti-proliferation effect. Further, the anti-migration effect of Her-LP-MET on BCSCs was superior to that of MET or LP-MET, and was enhanced when used in concert with doxorubicin (DOX). In a mouse model, Her-LP-MET combined with free DOX was more effective than free MET, free DOX, or Her-LP-MET. Moreover, Her-LP-MET combined with free DOX yielded tumor remission, whereas free DOX alone resulted in metastasis or death. As such, Her-LP-MET formulation is expected to provide a new therapeutic modality targeting BCSCs. View Full-Text
Keywords: Metformin; Herceptin; breast cancer stem cell; liposome; targeting Metformin; Herceptin; breast cancer stem cell; liposome; targeting
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MDPI and ACS Style

Lee, J.-Y.; Shin, D.H.; Kim, J.-S. Anticancer Effect of Metformin in Herceptin-Conjugated Liposome for Breast Cancer. Pharmaceutics 2020, 12, 11.

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