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

Seong Kyeong Kim; Jae Min Lee; Kyung Taek Oh; Eun Seong Lee

doi:10.1016/j.ijpharm.2017.05.068

Extremely small-sized globular poly(ethylene glycol)-cyclic RGD conjugates targeting integrin α_vβ₃ in tumor cells

Seong Kyeong Kim
, Jae Min Lee
, Kyung Taek Oh
, Eun Seong Lee

Department of Biomedical-Chemical Engineering

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

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 (3–4 nm 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 α_vβ₃ receptors) than in KB cells (which have a very low density of integrin α_vβ₃ 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.

Original language	English
Pages (from-to)	1-7
Number of pages	7
Journal	International Journal of Pharmaceutics
Volume	528
Issue number	1-2
DOIs	https://doi.org/10.1016/j.ijpharm.2017.05.068
State	Published - 7 Aug 2017

Bibliographical note

Publisher Copyright:
© 2017 Elsevier B.V.

Keywords

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

Access to Document

10.1016/j.ijpharm.2017.05.068

Cite this

@article{54c0a7f8e2e740c2a751909238ff686a,

title = "Extremely small-sized globular poly(ethylene glycol)-cyclic RGD conjugates targeting integrin αvβ3 in tumor cells",

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 (3–4 nm 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",

author = "Kim, \{Seong Kyeong\} and Lee, \{Jae Min\} and Oh, \{Kyung Taek\} and Lee, \{Eun Seong\}",

note = "Publisher Copyright: {\textcopyright} 2017 Elsevier B.V.",

year = "2017",

month = aug,

day = "7",

doi = "10.1016/j.ijpharm.2017.05.068",

language = "English",

volume = "528",

pages = "1--7",

journal = "International Journal of Pharmaceutics",

issn = "0378-5173",

publisher = "Elsevier B.V.",

number = "1-2",

}

TY - JOUR

T1 - Extremely small-sized globular poly(ethylene glycol)-cyclic RGD conjugates targeting integrin αvβ3 in tumor cells

AU - Kim, Seong Kyeong

AU - Lee, Jae Min

AU - Oh, Kyung Taek

AU - Lee, Eun Seong

PY - 2017/8/7

Y1 - 2017/8/7

N2 - 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 (3–4 nm 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.

AB - 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 (3–4 nm 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.

KW - Chlorin e6

KW - Cyclic arginine-glycine-aspartic acid (cRGD) peptide

KW - Globular poly(ethylene glycol)

KW - Photodynamic tumor therapy

UR - https://www.scopus.com/pages/publications/85019976223

U2 - 10.1016/j.ijpharm.2017.05.068

DO - 10.1016/j.ijpharm.2017.05.068

M3 - Article

C2 - 28571905

AN - SCOPUS:85019976223

SN - 0378-5173

VL - 528

SP - 1

EP - 7

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 1-2

ER -