Optimized nanoemulsifying systems with enhanced bioavailability of carvedilol

The current studies entail a novel approach of formulating the solid self-nanoemulsifying drug delivery systems (S-SNEDDS) of carvedilol solely using rational blends of lipidic and emulsifying excipients without using equipment-intensive techniques and/or inert porous carriers. Delineating the nanoemulsion regions, the amounts of Capmul MCM (i.e., lipid) and Nikkol HCO 50 (i.e., emulgent) were selected as the critical factors for systematically formulating the optimized S-SNEDDS employing face centered cube design. The optimized formulation (mean globule size: 40.8 nm) indicated marked improvement in drug release profile vis-à-vis pure drug and marketed formulation. Augmentation in the values of Cmax (134.2%) and AUC (85.2%) indicated significant enhancement in the rate and extent of bioavailability by the S-SNEDDS formulation compared to pure drug. In situ SPIP studies ascribed the significant enhancement in absorptivity parameters of SNEDDS formulations to transport through the lymphatic system and reduced P-gp efflux. Successful establishment of various levels of in vitro/in vivo correlations (IVIVC's) substantiated the judicious choice of the in vitro dissolution milieu for simulating the in vivo conditions. The optimized formulation was found to be quite stable during six months of study period. The current investigations, therefore, report the successful development of systematically optimized S-SNEDDS with enhanced bioavailability potential of carvedilol.

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► Novel approach for formulation of solid self nanoemulsifying drug delivery systems obviates the use of specialized machines and/or porous carriers.
► The optimized S-SNEDDS formulation possessed mean globule size of 40.8 nm.
► Augmentation in values of Cmax (134.2%) and AUC (85.2%) was observed.
► Various levels of IVIVC were established.
► Marked improvement in in situ perfusion profiles was observed.