Dual-responsive gemini micelles for efficient delivery of anticancer therapeutics

Young In Choi; Eun Sook Choi; Kwan Ho Mun; Se Guen Lee; Sung Jun Lee; Sang Won Jeong; Seung Woo Lee; Hyun Chul Kim

doi:10.3390/polym11040604

Dual-responsive gemini micelles for efficient delivery of anticancer therapeutics

Young In Choi, Eun Sook Choi, Kwan Ho Mun, Se Guen Lee, Sung Jun Lee, Sang Won Jeong, Seung Woo Lee, Hyun Chul Kim

Division of Biotechnology

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

4 Scopus citations

Abstract

Polymeric micelles as drug delivery vehicles are popular owing to several advantages. In this study, a gemini amphiphile (gemini mPEG-Cys-PMT) consisting of hydrophilic poly(ethylene glycol) and hydrophobic poly(methionine) with cystine disulfide spacer was synthesized and its micellar properties for thiol- or reactive oxygen species (ROS)-dependent intracellular drug delivery were described. The cleavage of cystine linkage in a redox environment or the oxidation of methionine units in a ROS environment caused the destabilization of micelles. Such redox- or ROS-triggered micellar destabilization led to enhanced release of encapsulated doxorubicin (DOX) to induce cytotoxicity against cancer cells. Further, the therapeutic effects of the DOX-loaded micelles were demonstrated using the KB cell line. This study shows that thiol and ROS dual-responsive gemini micelles are promising platforms for nano-drug delivery in various cancer therapies.

Original language	English
Article number	604
Journal	Polymers
Volume	11
Issue number	4
DOIs	https://doi.org/10.3390/polym11040604
State	Published - 1 Apr 2019

Bibliographical note

Publisher Copyright:
© 2019 by the authors.

Keywords

Disulfide-thiol exchange
Drug delivery systems
Gemini micelles
Reactive oxygen species

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3390/polym11040604

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title = "Dual-responsive gemini micelles for efficient delivery of anticancer therapeutics",

abstract = "Polymeric micelles as drug delivery vehicles are popular owing to several advantages. In this study, a gemini amphiphile (gemini mPEG-Cys-PMT) consisting of hydrophilic poly(ethylene glycol) and hydrophobic poly(methionine) with cystine disulfide spacer was synthesized and its micellar properties for thiol- or reactive oxygen species (ROS)-dependent intracellular drug delivery were described. The cleavage of cystine linkage in a redox environment or the oxidation of methionine units in a ROS environment caused the destabilization of micelles. Such redox- or ROS-triggered micellar destabilization led to enhanced release of encapsulated doxorubicin (DOX) to induce cytotoxicity against cancer cells. Further, the therapeutic effects of the DOX-loaded micelles were demonstrated using the KB cell line. This study shows that thiol and ROS dual-responsive gemini micelles are promising platforms for nano-drug delivery in various cancer therapies.",

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doi = "10.3390/polym11040604",

language = "English",

volume = "11",

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T1 - Dual-responsive gemini micelles for efficient delivery of anticancer therapeutics

AU - Choi, Young In

AU - Choi, Eun Sook

AU - Mun, Kwan Ho

AU - Lee, Se Guen

AU - Lee, Sung Jun

AU - Jeong, Sang Won

AU - Lee, Seung Woo

AU - Kim, Hyun Chul

PY - 2019/4/1

Y1 - 2019/4/1

N2 - Polymeric micelles as drug delivery vehicles are popular owing to several advantages. In this study, a gemini amphiphile (gemini mPEG-Cys-PMT) consisting of hydrophilic poly(ethylene glycol) and hydrophobic poly(methionine) with cystine disulfide spacer was synthesized and its micellar properties for thiol- or reactive oxygen species (ROS)-dependent intracellular drug delivery were described. The cleavage of cystine linkage in a redox environment or the oxidation of methionine units in a ROS environment caused the destabilization of micelles. Such redox- or ROS-triggered micellar destabilization led to enhanced release of encapsulated doxorubicin (DOX) to induce cytotoxicity against cancer cells. Further, the therapeutic effects of the DOX-loaded micelles were demonstrated using the KB cell line. This study shows that thiol and ROS dual-responsive gemini micelles are promising platforms for nano-drug delivery in various cancer therapies.

AB - Polymeric micelles as drug delivery vehicles are popular owing to several advantages. In this study, a gemini amphiphile (gemini mPEG-Cys-PMT) consisting of hydrophilic poly(ethylene glycol) and hydrophobic poly(methionine) with cystine disulfide spacer was synthesized and its micellar properties for thiol- or reactive oxygen species (ROS)-dependent intracellular drug delivery were described. The cleavage of cystine linkage in a redox environment or the oxidation of methionine units in a ROS environment caused the destabilization of micelles. Such redox- or ROS-triggered micellar destabilization led to enhanced release of encapsulated doxorubicin (DOX) to induce cytotoxicity against cancer cells. Further, the therapeutic effects of the DOX-loaded micelles were demonstrated using the KB cell line. This study shows that thiol and ROS dual-responsive gemini micelles are promising platforms for nano-drug delivery in various cancer therapies.

KW - Disulfide-thiol exchange

KW - Drug delivery systems

KW - Gemini micelles

KW - Reactive oxygen species

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U2 - 10.3390/polym11040604

DO - 10.3390/polym11040604

M3 - Article

AN - SCOPUS:85065907724

SN - 2073-4360

VL - 11

JO - Polymers

JF - Polymers

IS - 4

M1 - 604

ER -

Dual-responsive gemini micelles for efficient delivery of anticancer therapeutics

Abstract

Bibliographical note

Keywords

UN SDGs

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