In this study, double-hydrophilic hydroxylpropyl cellulose （HPC） based copolymers with poly（N- isopropylacrylamide） （PNIPAM） and poly（acrylic acid） （PAA） as graft chains were synthesized and characterized. T...In this study, double-hydrophilic hydroxylpropyl cellulose （HPC） based copolymers with poly（N- isopropylacrylamide） （PNIPAM） and poly（acrylic acid） （PAA） as graft chains were synthesized and characterized. The release behavior of drug-loaded micelles was studied. The results show that the hydrophilicity of copolymers improves as the pH increases, whereas the hydrophobicity of copolymers enhances as the temperature increases, and all the phase behaviors are reversible. The diameter of micelles decreases and then increases with pH increase. It shows different micellizing behavior under acidic and basic conditions according to the temperature increase. In vitro release experiments, which used theophylline as a model drug, show that the micelles enhance pH sensitivity in the release process.展开更多
In this study, two kinds of docetaxel （DTX）-loaded mixed micelles, composed of Solutol HS15 （HS 15）/Pluronic F127 （F 127） or folate-conjugated F127, （SF-DTX and FSF-DTX）, were prepared by the thin-film hydrati...In this study, two kinds of docetaxel （DTX）-loaded mixed micelles, composed of Solutol HS15 （HS 15）/Pluronic F127 （F 127） or folate-conjugated F127, （SF-DTX and FSF-DTX）, were prepared by the thin-film hydration method and evaluated in vitro. Both SF-DTX and FSF-DTX were spherical with diameter close to 23 nm. They had high encapsulating efficiency （99.05% and 90.28% for SF-DTX and FSF-DTX, respectively） and sustained-release property. SF and FSF were able to enhance the cellular accumulation of DTX in KBv cells and reduce ATP content in A-549 cells. They also were able to reverse multidrug resistance （MDR）. In vitro cytotoxicity and cellular accumulation of DTX suggested an active targeting of FSF-DTX. It could be concluded from the results that the novel F 127/HS 15 system could serve as a potential nanocarrier with the ability of overcoming MDR, and folate-conjugated F 127/HS 15 might achieve active targeting at the same time.展开更多
文摘In this study, double-hydrophilic hydroxylpropyl cellulose （HPC） based copolymers with poly（N- isopropylacrylamide） （PNIPAM） and poly（acrylic acid） （PAA） as graft chains were synthesized and characterized. The release behavior of drug-loaded micelles was studied. The results show that the hydrophilicity of copolymers improves as the pH increases, whereas the hydrophobicity of copolymers enhances as the temperature increases, and all the phase behaviors are reversible. The diameter of micelles decreases and then increases with pH increase. It shows different micellizing behavior under acidic and basic conditions according to the temperature increase. In vitro release experiments, which used theophylline as a model drug, show that the micelles enhance pH sensitivity in the release process.
基金The Key Disciplines Research Funds for the Young Teachers(Grant No.2013jzzdxk038)
文摘In this study, two kinds of docetaxel （DTX）-loaded mixed micelles, composed of Solutol HS15 （HS 15）/Pluronic F127 （F 127） or folate-conjugated F127, （SF-DTX and FSF-DTX）, were prepared by the thin-film hydration method and evaluated in vitro. Both SF-DTX and FSF-DTX were spherical with diameter close to 23 nm. They had high encapsulating efficiency （99.05% and 90.28% for SF-DTX and FSF-DTX, respectively） and sustained-release property. SF and FSF were able to enhance the cellular accumulation of DTX in KBv cells and reduce ATP content in A-549 cells. They also were able to reverse multidrug resistance （MDR）. In vitro cytotoxicity and cellular accumulation of DTX suggested an active targeting of FSF-DTX. It could be concluded from the results that the novel F 127/HS 15 system could serve as a potential nanocarrier with the ability of overcoming MDR, and folate-conjugated F 127/HS 15 might achieve active targeting at the same time.
