Drug Discovery and Development

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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.