Phosphatidylcholine Complex in Improving Oral Drug Delivery of Epicatechin: Preparation and Characterization

Abstract

Epicatechin, a polyphenolic flavonoid, shows antioxidant, anti-bacterial, anticarcinogenic and antitumour activity. Like other flavonoids, epicatechin is poorly absorbed across the gastrointestinal tract because it has multiple ring molecules that are too large to be absorbed by simple diffusion. It shows poor miscibility with oils and other lipids which limit its ability to pass across the lipid rich biomembranes of small intestine. Therefore, in an attempt to improve the problem of poor absorption, solubility and dissolution of epicatechin its phospholipid complexes were prepared. The prepared epicatechin-phospholipid complex was characterized for various physico-chemical parameters like drug loading, infrared absorption (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), aqueous/n-octanol solubility and dissolution study. In the SEM, the complex was observed as nonporous irregular particles with rough surface morphology. FTIR and DSC data confirmed the formation of phospholipid complex. The water and n-octanol solubility of epicatechin was improved from 326.32 to 427.12 μg/ml and 378.53 to 502.67 μg/ml, respectively in the complex. The dissolution was also improved significantly in the phospholipid complex. It was concluded that the phospholipid complex may be used for improving solubility, dissolution and hence the bioavailability of epicatechin molecule.