Glutathione-responsive gemini polymeric micelles as controlled drug carriers
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  • 作者:Hyun-Chul Kim (1)
    Eunjoo Kim (1)
    Sang Won Jeong (1)
    Se Guen Lee (1)
    Sung Jun Lee (1)
    Seung Woo Lee (2)

    1. Nano & Bio Research Division
    ; Daegu Gyeongbuk Institute of Science and Technology (DGIST) ; Daegu ; 711-873 ; Korea
    2. School of Chemical Engineering
    ; Yeungnam University ; Gyeongbuk ; 712-749 ; Korea
  • 关键词:gemini surfactants ; drug delivery system ; polypeptide ; disulfide ; thiol exchange ; stimuli ; sensitive polymers
  • 刊名:Macromolecular Research
  • 出版年:2015
  • 出版时间:February 2015
  • 年:2015
  • 卷:23
  • 期:2
  • 页码:196-204
  • 全文大小:749 KB
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  • 刊物类别:Chemistry and Materials Science
  • 刊物主题:Chemistry
    Physical Chemistry
    Polymer Sciences
    Characterization and Evaluation of Materials
    Soft and Granular Matter, Complex Fluids and Microfluidics
    Nanochemistry
    Nanotec
  • 出版者:The Polymer Society of Korea, co-published with Springer
  • ISSN:2092-7673
文摘
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.

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