Naringenin, a lipophilic flavanone of citrus fruits, was encapsulated for enhanced bioavailability using biodegradable polymers of polylactic acid/polyvinyl alcohol (PLA/PVA) as well as zein/pectin as P/P-Nar-NPs and Z/P-Nar-NPs, respectively. The formulation variables were optimized using response surface methodology to achieve smaller particle size with higher surface charge and encapsulation efficiencies. The optimized formulations were physically characterized by SEM, FTIR, TGA and XRD techniques. Compared to Z/P-Nar-NPs, the P/P-Nar-NPs had better encapsulation efficiency and sustained release of naringenin under simulated gastrointestinal conditions. Furthermore, the oral administration of single dose of free and nanoforms of naringenin in rats (90 mg/kg b.wt) showed higher efficacy of PLA/PVA in improving the relative bioavailability of naringenin (4.7-fold) as compared to the zein/pectin polymer (1.9-fold). Overall, the present study provides insights into the formulation performance of the encapsulated bioactive compound under different polymeric matrices.
Keywords: Bio-distribution; Bioflavonoid; In-vitro release; Nano-encapsulation; Pharmacokinetics; Response surface methodology.
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