ENHANCEMENT OF SOLUBILITY AND DISSOLUTION PROFILE OF EPLERENONE BY LIQUISOLID COMPACTS USING NOVEL EXCIPIENTSAbstract
Eplerenone is a poorly soluble drug that belongs to class II biopharmaceutical classification system. It is a selective aldosterone receptor antagonist, which binds to the mineralocorticoid receptor and blocks the binding of aldosterone, thereby decreases the sodium resorption and subsequently increasing water outflow. This leads to a decrease in blood pressure and used in congestive heart failure. The aim of the present study was to improve the solubility, dissolution and permeability properties of Eplerenone by liquisolid compacts, thereby enhancing oral bioavailability. Different formulations of Liquisolid were developed by dissolving the drug in mixture of Transcutol HP: Capmul MCM and Cremophor EL: Capmul MCM (Non-volatile liquid; 1:1 ratio), converting this liquid medication using carriers as fujicalin and neusilin and coating material as syloid FP 244. The results showed that Liquisolid formulation exhibited significantly higher drug dissolution rate compared to pure drug as well as marketed formulation. The plasma concentration-time profile of healthy Wister rats indicated that the oral bioavailability of optimized formulation has been significantly improved compared to pure drug and marketed formulation. The enhanced bioavailability might be due to increased wetting properties of drug and permeability of the drug due to lipophilic properties of solvent used for wetting. This study can conclude that Liquisolid technique is a promising alternative method for improving the bioavailability of class-II drugs.