PEG-Stabilized Micellar System with Positively Charged Polyester Core for Fast pH-Responsive Drug Release

作者: Hua-Fen Wang , Hui-Zhen Jia , Si-Xue Cheng , Jun Feng , Xian-Zheng Zhang

DOI: 10.1007/S11095-012-0669-9

关键词: ChemistryDrug carrierMorphology (linguistics)PEG ratioEthylene glycolTertiary aminePolyesterCopolymerMicellePolymer chemistry

摘要: To design functional drug carriers for fast pH-responsive release. Functional diblock terpolymers of monomethoxy poly(ethylene glycol)-block- copoly(6,14-dimethyl-1,3,9,11-tetraoxa-6,14-diaza-cyclohexadecane-2,10-dione-co-e-caprolactone) [mPEG-b-poly(ADMC-co-CL)] were fabricated via biosynthetic pathway. The self-assembled nanosphere and drug-loaded micelles the copolymers further prepared by dialysis method. pH-tunable morphology variation release pattern observed at different pH. A collection three PEGylated with varied compositions in poly(ADMC-co-CL) block was designed high cell-biocompatibility. could readily self-assemble into nanoscale (~ 100 nm) aqueous medium exhibit stability over 80-h incubation mediums including deionized water, neutral NaCl solution, heparin sodium solution. Due to protonation-deprotonation tertiary amine groups ADMC units, acid-induced structural deformation disclosed terms CAC value hydrodynamic size Drug loading efficiency comparable that reported PEG-polyester specifically structures purposed drug-loading improvement. Remarkably accelerated triggered acidity distinctly detected ibuprofen-loaded mPEG-b-poly(ADMC-co-CL) micelle system, suggesting a characteristic. PEG-stabilized micellar positively charged polyester core successfully developed

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