In vitro characterization of pH-sensitive azithromycin-loaded methoxy poly (ethylene glycol)-block-poly (aspartic acid-graft-imidazole) micelles
| Autor: | Runliang Feng, Peizong Deng, Fangfang Teng, Zhimei Song, Na Liu, Feilong Zhou |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Staphylococcus aureus
02 engineering and technology Azithromycin 010402 general chemistry 01 natural sciences Micelle Polyethylene Glycols Biomaterials chemistry.chemical_compound Colloid and Surface Chemistry Zeta potential Copolymer Organic chemistry Imidazole Particle Size Micelles Aspartic Acid Drug Carriers Chemistry Imidazoles Hydrogen-Ion Concentration 021001 nanoscience & nanotechnology 0104 chemical sciences Surfaces Coatings and Films Electronic Optical and Magnetic Materials Polymerization Drug delivery 0210 nano-technology Antibacterial activity Ethylene glycol Nuclear chemistry |
| Zdroj: | Journal of Colloid and Interface Science. 496:16-25 |
| ISSN: | 0021-9797 |
| Popis: | In order to improve azithromycin's antibacterial activity in acidic medium, monomethoxy poly (ethylene glycol)-block-poly (aspartic acid-graft-imidazole) copolymer was synthesized through allylation, free radical addition, ring-opening polymerization and amidation reactions with methoxy poly (ethylene glycol) as raw material. Drug loading capacity and encapsulation efficiency of azithromycin-loaded micelles prepared via thin film hydration method were 11.58±0.86% and 96.06±1.93%, respectively. The drug-loaded micelles showed pH-dependent property in the respects of particle size, zeta potential at the range of pH 5.5-7.8. It could control drug in vitro release and demonstrate higher release rate at pH 6.0 than that at pH 7.4. In vitro antibacterial experiment indicated that the activity of azithromycin-loaded micelles against S. aureus was superior to free azithromycin in medium at both pH 6.0 and pH 7.4. Using fluorescein as substitute with pH-dependent fluorescence decrease property, laser confocal fluorescence microscopy analysis confirmed that cellular uptake of micelles was improved due to protonation of copolymer's imidazole groups at pH 6.0. The enhanced cellular uptake and release of drug caused its activity enhancement in acidic medium when compared with free drug. The micellar drug delivery system should be potential application in the field of bacterial infection treatment. |
| Databáze: | OpenAIRE |
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