Formulation Development of Porous Mannitol carrier: Improving the dissolution of poorly soluble drugs

Abstract

Major challenges in the design of oral dosage forms are their low solubility and low bioavailability. Improving the dissolution of these oral dosage forms are one of the most challenging tasks for the formulation scientists as most of the drug candidates are highly lipophilic in nature. Telmisartan and Ezetimibe belongs to the BCS class II, having high lipophilicity, poor water solubility and poor dissolution. The objective of this work was to improve the dissolution rate of poorly water soluble drugs by using porous carrier drug delivery system. Templating based spray drying methodology was used to prepare porous mannitol. Drug (Telmisartan, Ezetimibe) loaded porous mannitol carriers then characterized by P-XRD, DSC, SEM, BET surface area analysis and ATR-FTIR. ATR-FTIR studies showed complete removal of templating agent from carrier. P-XRD and DSC studies confirmed nano- confinement of drug in crystalline form. In vitro dissolution study results indicated that porous mannitol prepared using tartaric acid as templating agent showed significant improvement in dissolution rate than pure drugs and respective physical mixtures .These results suggest that, these porous carriers can be useful as drug carriers for improving the dissolution of lipophilic drugs.
 Keywords: Templating agent, Spray drying, Mannitol, Surface area, Tartaric acid.