Purpose:
The purpose of this study is to develop a new PLGA based formulation for microspheres, which aims to
release mometasone furoate for one month, so as to improve compliance.
Methods:
The microspheres containing mometasone furoate were prepared by oil in water emulsion and solvent evaporation. The microspheres were characterized by surface morphology, shape, size and encapsulation efficiency. The release in
vitro was studied in 37°C phosphate buffer, and in vivo, pharmacodynamics and preliminary safety evaluation were conducted in male Sprague Dawley rats.
Results:
The morphology results show that the microspheres have smooth surface, spherical shape and the average diameter
of 2.320-5.679μm. The encapsulation efficiency of the microspheres loaded with mometasone furoate is in the range of
53.1% to 95.2%, and the encapsulation efficiency of the microspheres can be greatly affected by the proportion of oil phase
to water phase and other formulation parameters. In vitro release kinetics revealed that drug release from microspheres was
through non Fick's diffusion and PLGA polymer erosion. Pharmacokinetic data showed that the initial release of microspheres was small and then sustained. The results of pharmacodynamic study fully proved the effectiveness and long-term
effect of mometasone furoate microspheres. The results of in vivo safety evaluation showed that the preparation system had
good in vivo safety.
Conclusion:
This study shows that the microspheres prepared in this study have sufficient ability of stable drug release at
least 35 days, with good efficacy and high safety. In addition, mometasone furoate can be used as a potential candidate drug
for 35 day long-term injection.
In vivo and in vitro efficacy of florfenicol, terbinafine, and mometasone furoate topical otic solution for the treatment of canine otitis externa
