Biocompatible nanocarriers of bioactive flavonoid naringin: Design, formulation, and comprehensive characterization

Naringin (NAR), a citrus flavonoid has been reported to have anti-inflammatory, antitumor, antiviral, antiadipogenic, and cardioprotective qualities. However, because of its poor aqueous solubility, therapeutic applications of NAR are limited. The present research involves development of nanocarriers of NAR using biocompatible natural polymer chitosan and tripolyphosphate using ionic gelation method. Surface morphology studies indicated the structure of the prepared nanocarriers with an entrapment of more than 80% and appreciable average size range of around 100 nm. Drug release studies suggested that the drug released at a controlled manner with around of around 65% over a period of 6 hours with a burst release of around 20% in the first hour. 3-(4, 5-dimethythiazol2-yl)-2, 5-diphenyl tetrazolium bromide test using HEK 293 cells demonstrated that highest concentration of NAR loaded nanocarriers (100 μM) showed optimal viability and cells were not harmed by nanocarriers. In-vivo anti-inflammatory activity study suggested that prepared formulation (50 mg/kg) significantly reduced development of carrageenan induced paw edema, comparable with diclofenac treated rats (10 mg/kg) but significantly enhanced for rats treated with NAR only (50 mg/kg). Together, the results suggested that chitosan based nanocarriers could be an efficient tool to deliver naringin thus ensuring better bioavailability to enhance its therapeutic potential.