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
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.
