Enhancement Solubilization of Dutasteride using Microsponge Formulation

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Hassanien S. Taghi
Mustafa R. Abdulbaqi
Esraa G. Jabar

Abstract

Dutasteride (DU) (5α-reductase inhibitor) that is used for the treatment of benign prostate hyperplasia (BPH), DU has low water solubility and poor oral absorption that classified as Biopharmaceutics Classification System (BCS) class II.
This study aims to improve the physical properties of Dutasteride (DU) like solubility by the preparation of microsponge (MS). Microsponges are spherical in shape, sponge-like structure, polymeric delivery systems composed of porous microspheres with a large internal surface area. Nine formulations of DU MS had been prepared by the technique of quasi-emulsion solvent diffusion(QESD) and utilizing Eudragit S100 as major polymer and glycerol as a plasticizer that dissolved in dichloromethane where polyvinyl alcohol PVA serves as a stabilizer in the external phase.
The formulas were employed to optimize preparation variable factors include; different drug to polymer ratio, the addition of different concentrations of PVA, and stirring rate. Optimization was done using the response of production yield (PY), entrapment efficiency EE), particle size, and in vitro drug release; The results display that the best ratio of (drug: polymer) was 5:1, and the best rate of stirring was 1000 rpm respecting the optimum characteristics of microsponge. The best-selected formula prepared (F2) was underwent to evaluation regarding saturated solubility, FTIR, DSC, and SEM and showed 1.28 folds enhancement in saturated solubility compared to plain DU, and was well fabricated with high entrapment efficiency (83.7% ± 1.37), production yield (85.61% ± 0.6), and particle size of 77μm. Moreover, the percent release of DU was 75.74 ± 1.5 after 4 hours., with good compatibility as confirmed by XRD, SEM, DSC, and FTIR analysis.
It can be concluded that the selected formula prepared (F2) of DU microsponge is reassuring and promising drug delivery with improved pharmaceutical physical properties.

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Research Article