Emad B. Basalious
Cairo University, Egypt
Title: Self-nanoemulsifying self-nanosuspension (SNESNS) for enhancing oral bioavailability of diacerein: Simultaneous portal blood absorption and lymphatic delivery
Biography
Biography: Emad B. Basalious
Abstract
The application of self-Nano emulsified drug delivery system (SNEDDS) to improve bioavailability of diacerein (D) has been hampered by its large dose and limited solubility. This work aimed to prepare diacerein loaded self-Nano emulsifying self-Nano suspension (D-SNESNS) containing high drug load. DSNESNS was prepared by homogenizing D into MaisineTM-based SNEDDS that gave the highest drug solubility. D-SNESNS was evaluated for particle size, zeta potential and in vitro dissolution. Significant increase of D solubility was observed from D-SNESNS ( 309 mg/mL) than traditional SNEDDS (162 mg/mL) due to the spontaneous simultaneous formation of Nanoemulsion and Nano suspension (top–down approach). When exposed to water with mild agitation, the drug micro particles in D-SNESNS are temporarily surrounded by unsaturated aqueous layer (containing optimum concentrations of surfactant and co-solvent) that facilitates the erosion of the suspended drug particles into Nano sized ones. Nanoemulsion-based nano suspension (NENS) was confirmed using transmission electron microscopy and particle size analysis. D-SNESNS equivalent to 50 mg D exhibited complete and very rapid dissolution after 15 min in phosphate buffer pH 6.8 due to the existence of D as solubilized molecules inside Nanoemulsion globules and Nano sized suspended drug particles forming D-NENS. The relative bio availabilities of rhein from D-SNESNS in rats with normal and blocked chylomicron flow were about 210% and 164%, respectively in comparison to aqueous D suspension. The significant increase in the dissolution, portal absorption and lymphatic delivery of D propose that SNESNS could be promising to improve oral bioavailability of poorly water soluble drugs that have limited drug load in SNEDDS.