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Glutathione-Responsive Gemini Polymeric Micelles as Controlled Drug Carriers
- Glutathione-Responsive Gemini Polymeric Micelles as Controlled Drug Carriers
- Kim, Hyun-Chul; Kim, Eunjoo; Jeong, Sang Won; Lee, Se Guen; Lee, Sung Jun; Lee, Seung Woo
- DGIST Authors
- Kim, Hyun-Chul; Kim, Eunjoo; Jeong, Sang Won; Lee, Se Guen; Lee, Sung Jun
- Issue Date
- Macromolecular Research, 23(2), 196-204
- Article Type
- Amino Acids; Controlled Drug Delivery; Covalent Bonds; Critical Micelle Concentration (CMC); Cystines; Cytotoxicity; Disulfide-Thiol Exchange; Disulfide-Thiol Exchanges; Drug Delivery; Drug Delivery System; Drug Products; Gemini Surfactant; Gemini Surfactants; GSH Concentrations; Intracellular Compartments; Loading; Micelles; Microscopic Observations; Peptides; Polyethylene Glycols; Polymers; Polyols; Polypeptide; Polypeptides; Stimuli-Sensitive Polymers; Sulfur Compounds
- Gemini poly(ethylene glycol)-cystine-poly(s-butyl cysteine) ((PEG)2-Cyt-(PBC)2) with a cystine disulfide bond as a spacer was prepared via oxidation of the cysteine group of monomeric poly(ethylene glycol)-cysteine-poly(s-butyl cysteine) (PEG-Cys-PBC) in solution, which is specifically cleavable in intracellular compartments. Due to its amphiphilic nature, (PEG)2-Cyt-(PBC)2 formed micelles under aqueous conditions; the average diameter of the micelles was 26.9 nm. The critical micelle concentration (CMC) of the polymer was 15.8 mg/L. The loading content of the chosen model drug, indomethacine (IMC), was much higher for gemini micelles than that for monomeric micelles. The (PEG)2-Cyt-(PBC)2 micelles released 75% of the loaded IMC within 72 h under 10 mM glutathione (GSH), whereas 36% of the loaded IMC was released from the micelles in the absence of GSH. An in vitro cytotoxicity experiment revealed that PTX-loaded gemini micelles showed toxicity to A549 cells with increasing GSH concentrations. Microscopic observation of gemini micelles demonstrated that the micelles containing a disulfide bond could effectively deliver the drug into A549 cells. These results suggest the potential of disulfide-based gemini polymeric micelles as controlled drug delivery carriers.[Figure not available: see fulltext.] © 2015, The Polymer Society of Korea and Springer Sciene+Business Media Dordrecht.
- Polymer Society of Korea
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