Competence of raloxifene hydrochloride loaded liquisolid compacts for improved dissolution and intestinal permeation

• Published in: Journal of drug delivery science and technology 2015-12, Vol.30, p.232-241
• Main Authors: Komala, Devender Reddy, Janga, Karthik Yadav, Jukanti, Raju, Bandari, Suresh, Vijayagopal, M.
• Format: Article
• Language: English
• Subjects: Dissolution; Ex-vivo permeation; Liquid retention potential; Liquisolid compacts; Non-volatile liquids; Raloxifene HCl
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2015.10.020

The primary purpose of this research is to formulate raloxifene hydrochloride (RXH) loaded liquisolid compacts for improved dissolution behavior and intestinal permeation. Owing to their higher drug solubility, Cremophor® EL, Capmul PG-8 and Transcutol P were selected as suitable non-volatile liquid vehicles to develop desired formulations. The liquisolid formulations were obtained by allowing liquid vehicles with varying drug concentrations to get absorbed onto carrier and coating material taken at different ratios (R = 5; R = 10). Avicel PH 102 and Aerosil PH 200 displayed good liquid retention potential values confirming appropriate load factor and thus, resulting in liquisolid powders with good flow properties exemplifying their caliber as efficient solid carrier and coating materials in developing liquisolid compacts. FT-IR spectra illustrated no significant interaction between drug and carrier. The DSC and PXRD studies demonstrated the absence of crystalline form of drug in liquisolid powders. Further, the enhanced dissolution performance of RXH from liquisolid systems suggested the transformation of the drug to molecular/amorphous state. Ex vivo rat intestinal permeation studies revealed an improvement in drug absorption from formulation unraveling the ability of non-volatile liquid vehicles of liquisolid systems in enhancing the intestinal permeation of dissolution rate limited RXH. [Display omitted]