Dual-responsive Gemini Micelles for Efficient Delivery of Anticancer Therapeutics

• Published in: Polymers Vol. 11; no. 4; p. 604
• Main Authors: Choi, Young In, Choi, Eun-Sook, Mun, Kwan Ho, Lee, Se Guen, Lee, Sung Jun, Jeong, Sang Won, Lee, Seung Woo, Kim, Hyun-Chul
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 02-04-2019; MDPI
• Subjects: Cancer; Chromatography; Cystine; Destabilization; disulfide–thiol exchange; Doxorubicin; Drug delivery systems; gemini micelles; Hydrogen peroxide; Methionine; Micelles; Molecular weight; Nanoparticles; NMR; Nuclear magnetic resonance; Oxidation; Phase transitions; Polyethylene glycol; Polymers; reactive oxygen species; Spectrum analysis; Toxicity; drug delivery systems; disulfide–thiol exchange; gemini micelles; reactive oxygen species
• ISSN: 2073-4360; 2073-4360
• DOI: 10.3390/polym11040604

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.