Preparation and characterization of phospholipid complexes of naringenin for effective drug delivery

Abstract

Naringenin is a flavonoid specific to citrus fruits and possesses anti-inflammatory, anticarcinogenic, and antitumour effects. But due to a lower half-life and rapid clearance from the body, frequent administration of the molecule is required. To improve the bioavailability and prolong its duration in body system, its phospholipid complexes were prepared by a simple and reproducible method. Naringenin was complexed with phosphatidylcholine in equimolar ratio, in presence of dichloromethane. The prepared Phytosomes (naringenin–phospholipid complex) were evaluated for various physical parameters like FT-IR spectroscopy, Differential Scanning Calorimetry (DSC), X-ray powder diffractometry (XRPD), Solubility, Scanning Electron Microscopy (SEM) and the in vitro drug release study. These phospholipid complexes of naringenin were found to be irregular and disc shaped with rough surface in SEM. Drug content was found to be 91.7% (w/w). FTIR, 1H NMR, DSC and XRPD data confirmed the formation of phospholipid complex. Water solubility of naringenin improved from 43.83 to 79.31 μg/mL in the prepared complex. Unlike the free naringenin (which showed a total of only 27% drug release at the end of 10 h), naringenin complex showed 99.80% release at the end of 10 h of dissolution study. Thus it can be concluded that the phospholipid complex of naringenin may be of potential use for improving bioavailability.