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Int J Pharm. 2017 Aug 7;528(1-2):1-7. doi: 10.1016/j.ijpharm.2017.05.068. Epub 2017 May 30.

Extremely small-sized globular poly(ethylene glycol)-cyclic RGD conjugates targeting integrin αvβ3 in tumor cells.

Author information

1
Department of Biotechnology, The Catholic University of Korea, 43-1 Yeokgok 2-dong, Wonmi-gu, Bucheon, Gyeonggi-do 420-743, Republic of Korea.
2
College of Pharmacy, Chung-Ang University, 221 Heukseok dong, Dongjak-gu, Seoul 155-756, Republic of Korea. Electronic address: kyungoh@cau.ac.kr.
3
Department of Biotechnology, The Catholic University of Korea, 43-1 Yeokgok 2-dong, Wonmi-gu, Bucheon, Gyeonggi-do 420-743, Republic of Korea. Electronic address: eslee@catholic.ac.kr.

Abstract

In this study, we report an extremely small-sized globular poly(ethylene glycol) (gPEG) conjugated with cyclic arginine-glycine-aspartic acid (cRGD) peptide and chlorin e6 (Ce6). This nanoparticle design takes advantage of the biocompatible functional gPEG (3-4nm in diameter) as an extremely small-sized drug carrier, the tumor targeting ability of cRGD, and the photodynamic tumor ablation ability of Ce6. We found that gPEG conjugated with cRGD and Ce6 (cRGD-gPEG-Ce6) exhibited much higher phototoxicity in SKOV-3 tumor cells (which have a very high density of integrin αvβ3 receptors) than in KB cells (which have a very low density of integrin αvβ3 receptors). Accordingly, cRGD-gPEG-Ce6 treatment resulted in a significant regression of in vivo SKOV-3 tumors, highlighting the potential of an extremely small-sized drug carrier platform for site-specific receptor-mediated tumor therapy.

KEYWORDS:

Chlorin e6; Cyclic arginine-glycine-aspartic acid (cRGD) peptide; Globular poly(ethylene glycol); Photodynamic tumor therapy

PMID:
28571905
DOI:
10.1016/j.ijpharm.2017.05.068
[Indexed for MEDLINE]

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