Pickering Dry Emulsion System for Improved Oral Delivery of Fenofibrate.

The current study reports a Pickering dry emulsion (PDE) system for improved oral delivery of fenofibrate, a poorly water-soluble model drug. The silica nanoparticles were modified by surface modifiers and explored as a stabilizer for emulsion. The wetting property of modified silica nanoparticles was evaluated by contact angle study. Emulsion was spray-dried to obtain PDE. PDE was evaluated for particle size analysis, drug loading, TGA, DSC, XRPD, FEG-SEM, in vitro dissolution study, and in vivo pharmacodynamic study. The particle size of liquid emulsion was found within the range of 0.3-0.6 µm; after spray drying, the particles agglomerated and exhibited an increase in particle size (1.5 µm). The high drug loading (13% w/w) was found in PDE. DSC and XRD study confirmed the amorphous form of fenofibrate. SEM study showed the formation of a spherical porous microcapsule structure. In vitro dissolution exhibited significant enhancement in drug release for the PDE system as compared to plain fenofibrate. The PDE significantly lowered serum lipid level as compared to plain fenofibrate in a Triton-based hypercholesterolemia model in rats, which ultimately confirmed the enhancement in bioavailability. Thus, the PDE system has good potential in the drug delivery area.

Supercritical processed starch nanosponge as a carrier for enhancement of dissolution and pharmacological efficacy of fenofibrate.

In current study, supercritical processed starch nanosponge (SSNS) used as a carrier for poorly water soluble drug (fenofibrate) to enhance its in-vitro and in-vivo performance. SSNS was prepared by using sol- gel method and effective supercritical drying technique. Fenofibrate was loaded into the SSNS by using solvent immersion method with selected and optimized organic solvent. BET surface area of SSNS was evaluated by nitrogen adsorption/desorption analysis. SSNS and drug loaded SSNS were characterized by DSC, XRPD, FTIR, SEM, Contact angle study and evaluated for in-vitro, in-vivo studies. The results revealed that the formed SSNS material has high surface area (180m2/gm) with pore size (40 nm to 200nm). The DSC and XRPD study revealed the amorphization of drug within a SSNS. SEM study showed the continuous porous structure with differ nanosized pores of SSNS. Contact angle study showed improvement in aqueous wetting property of drug within a SSNS. In-vitro drug release study showed remarkable dissolution enhancement of SSNS formulation as compared to plain drug. In vivo pharmacodynamic study (hyperlipidaemia model) showed SNSS based formulation significantly improved the bioavailability of drug. Thus SSNS carrier system has good potential to be explored as a delivery system for poorly water soluble drugs.

Dodecylamine Template-Based Hexagonal Mesoporous Silica (HMS) as a Carrier for Improved Oral Delivery of Fenofibrate.

The aim of present investigation was the preparation of dodecylamine template-based hexagonal mesoporous silica (HMS) as a carrier for poorly water-soluble drug (fenofibrate). HMS material has distinctive characteristics such as easy synthesis, high surface area and wormhole pores. These characteristics are highly admirable to make use of it as a carrier in drug delivery system. HMS was prepared by pH and temperature-independent process. Fenofibrate was loaded into the HMS by solvent immersion method using organic solvent. The BET surface area of HMS was evaluated by nitrogen adsorption/desorption analysis. HMS and drug-loaded HMS were characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and contact angle study. The HMS-based system was also evaluated for in vitro and in vivo study as compared to plain drug. The BET surface area of HMS was found 974 m2/g with a narrow pore size average of 2.6 nm. The DSC and XRD study confirmed the amorphization of drug within the HMS. SEM and TEM study showed morphological features of HMS as well as revealed the wormhole porous structure. Contact angle study showed improvement in aqueous wetting property of drug within the HMS (contact angle 46°). The In vitro drug release study showed a remarkable dissolution enhancement in HMS-based system as compared to plain drug. In vivo pharmacodynamic study (hyperlipidaemia model) exhibited HMS-based formulation was significantly improved the bioavailability of fenofibrate. Thus, HMS has admirable properties; makes it a potential carrier for delivery system of poorly water-soluble drugs.