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Colloids Surf B Biointerfaces. 2018 Oct 1;170:718-728. doi: 10.1016/j.colsurfb.2018.07.013. Epub 2018 Jul 7.

Folate receptor-mediated celastrol and irinotecan combination delivery using liposomes for effective chemotherapy.

Author information

1
College of Pharmacy, Yeungnam University, 214-1, Dae-dong, Gyeongsan, 712-749, Republic of Korea.
2
Department of Pharmaceutical Engineering, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, 31116, Republic of Korea.
3
College of Korean Medicine, Daegu Haany University, Gyeongsan, 712-715, Republic of Korea.
4
College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong Dongjak-gu, Seoul, 156-756, Republic of Korea.
5
College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, 426-791, Republic of Korea.
6
College of Pharmacy, Yeungnam University, 214-1, Dae-dong, Gyeongsan, 712-749, Republic of Korea. Electronic address: csyong@yu.ac.kr.
7
College of Pharmacy, Yeungnam University, 214-1, Dae-dong, Gyeongsan, 712-749, Republic of Korea. Electronic address: jongohkim@yu.ac.kr.

Abstract

Drug targeting using functionalized nanoparticles provides a new standard in anticancer therapy. Liposomes, safe and effective drug delivery carriers, can incorporate both hydrophilic and hydrophobic drugs for combination chemotherapy treatment of cancers. The objectives of the current study were to synthesize and test the effectiveness of a nanotechnology-based strategy utilizing folic acid (FA)-conjugated liposomes that incorporate both celastrol (Cs) and irinotecan (Ir) for targeted breast cancer therapy. Our results revealed the successful preparation of Cs and Ir-loaded folate-targeted liposomes (Lipo/Cs/Ir-FA) with a small particle size (∼190 nm) and polydispersity index (∼0.10). The formulation exhibited higher drug release profiles for both Ir and Cs at pH 5.0 compared to those at physiological pH, favoring cancer cell-targeted release. Furthermore, in vitro cell studies showed high uptake and enhanced apoptosis in folate receptor-positive breast cancer cells (MCF-7 and MDA-MB-231), but not in folate receptor-negative lung cancer cells (A549). Moreover, an in vivo study in a mouse tumor model using MDA-MB-231 xenografts supported effective drug delivery behavior of the folate-conjugated liposomes by selective targeting of tumor tissue and minimizing systemic adverse effects. Therefore, our formulation could provide an effective therapy for targeted cancer treatment.

KEYWORDS:

Breast cancer; Celastrol; Folic acid; Irinotecan; Liposomes

PMID:
30005409
DOI:
10.1016/j.colsurfb.2018.07.013
[Indexed for MEDLINE]

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