Novel self-nanoemulsifying self-nanosuspension (SNESNS) for enhancing oral bioavailability of diacerein: Simultaneous portal blood absorption and lymphatic delivery.

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