Self-microemulsifying systems of Finasteride with enhanced oral bioavailability: multivariate statistical evaluation, characterization, spray-drying and in vivo studies in human volunteers

Abstract

Aim: To develop Finasteride-loaded self micro-emulsifying drug delivery systems (SMEDDS) for the treatment of hormonal associated problems. Materials & methods: Ternary phase diagrams were constructed to obtain self-emulsification regions. Multivariate statistical methods viz. Principal component analysis and agglomerative hierarchy clustering analysis were used to evaluate the microemulsions stability. In vitro redispersibility study was adopted and two formulations were selected for spray-drying. Further investigations were performed (Fourier transform infrared, x-ray diffraction and transmission electron microscopy). Finally, the in vivo performance was tested in human volunteers. Results: Multivariate statistical methods selected stable SMEDDS. Spray-drying utilizing maltodextrin/leucin carrier system yielded a flowable product. Selected solid SMEDDS scored 129.35% relative bioavailability compared with a commercial tablet. Conclusion: The developed SMEDDS poses successful platform for glucosteroid analogs oral delivery. [Formula: see text]