Study of physicochemical properties of flutamide-loaded Ocimum basilicum microspheres with ex vivo mucoadhesion and in vitro drug release

ABSTRACT

Drug which shows extensive first pass effect is difficult task that, needs to be solved by formulators in the pharmaceutical science. The low oral bioavailability (49%) of flutamide may be due to poor wettability, low aqueous solubility and extensive first pass effect. The aim of present investigation was to prepare flutamide loaded microspheres and incorporate it into suppositories for rectal delivery to avoid first pass effect and enhance residence time. Flutamide loaded mucoadhesive microspheres of Ocimum Basilicum mucilage (OBM) were prepared using spray drying and characterized by percent production yield, encapsulation efficiency, particle size, zeta potential, polydispersity index, DSC, SEM, XRPD, in vitro drug release and stability studies. Moreover, ex vivo mucoadhesion was investigated using falling liquid film technique to determine the adhesion of microspheres to sheep rectal mucosa. The microspheres had nearly spherical shape and size about 2.53 μm. The encapsulation efficiency and mucoadhesion of optimized formulation MBF10 were found to be 69.6 ± 2.3% and 89.01 ± 2.18%, respectively. Percent CDR of optimized flutamide loaded mucoadhesive microspheres was found to be 88.7 ± 1.3 at 7 h. In conclusion, OBM microparticles based suppository could be used to deliver drug through rectal delivery.

KEYWORDS:

• Flutamide
• first pass effect
• mucoadhesive microspheres
• ocimum basilicum
• rectal drug delivery

Acknowledgments

The authors are grateful to Cipla Pharmaceutical Ltd, Bombay, India for gift sample of flutamide. Authors are thankful to University Grants Commission for minor research Grant (47-843/13(WRO) dated February 20, 2015