Wang Yu-zh
2014
Citations
0
Influential Citations
0
Citations
Quality indicators
Journal
Chinese Journal of Pharmaceutics
Abstract
Objective To prepare a kind of microemulsion thermosensitive in situ gel(ME-TISG) with nifeviroc(NFVR)as a model drug, and to explore its pharmaceutical properties. Methods Nifeviroc microemulsion(NFVR/ME) were prepared by temperature(75℃) control phase diagram and loaded into P407 gel. The particle size, ζ potential and morphology of the ME were analyzed by ZetePALS Zeta Potential Analyzer and Transmission Electron Microscope, and the rheology property was determined by Senior rotary rheometer. The correlation between NFVR/ME release and gel dissolution under a frequency of 100 r·min-1 was studied using non-membrane model. Results Average particle size of different concentration NFVR/ME was 36.30-38.25 nm and ζ potential was-7.15--7.22 mV. It showed that the micromorphology of ME was in round flat sphere shape. Sol-gel transition temperature and gelation temperature of the TISG was 29.5℃ and 34.5℃ respectively. NFVR/ME-TISG appeared to be newtonian fluid at low temperature(25℃) with low viscosity. The viscosity of ME increased as temperature rose and it showed a typical pseudoplastic fluid characteristics as to 35-37℃. The complex viscosity decreased gradually with the increase of shear rate, suggesting a shear-thinning behavior. In vitro release rate of NFVR was controlled by gel dissolution rate with good linear relationship(R2=0.98), following the zero order kinetics. Such gel dissolution-controlling drug release mode can avoid burst release effect. Conclusion ME-TISG is a promising new vaginal drug delivery system.