Formulation and Evaluation of Fenofibrate Dry Emulsion Tablets by Freeze Drying Method

Abstract

Fenofibrate (FF) is a lipid-lowering agent classified in the biopharmaceutics classification system (BCS) class II with lower solubility and higher permeability. This research work deals with developing FF containing liquid self-micro emulsifying drug delivery system (L-SMEDDS) and converting it into solid SMEDDS (S-SMEDDS) using a lyophilization technique followed by the manufacturing of tablets with enhanced solubility and dissolution rate. L-SMEDDS of FF were manufactured using Tween 80, oleic acid, and transcutol. With the help of the lyophilization technique, this L-SMEDDS was converted to S-SMEDDS using microcrystalline cellulose and finally, immediate-release tablets were developed using S-SMEDDS. The L-SMEDDS showed excellent stability due to zeta potential of -1.69 mV and a globule size of 250 μm. The lyophilized S-SMEDDS of FF showed nearly 58-fold solubility enhancement in distilled water in comparison to pure FF due to the formation of amorphous material confirmed in the X-ray diffraction (XRD) study. The F9 formulation showed 100% drug release within 40 minutes with enhanced dissolution properties compared to conventional tablets. The optimized formulation was robust and stable at the accelerated condition for 3 months. The current research work demonstrates lyophilization as a potential approach to convert the L-SMEDSS to a S-SMEDDS with an enhanced solubility and dissolution rate.