Enhanced hepatoprotective activity of andrographolide complexed with a biomaterial.

CONTEXT: Humic acid (HA), a natural organic matter is recently being investigated for pharmaceutical purposes. Andrographolide (AGP), a potent hepatoprotective, possesses low aqueous solubility which results in a low bioavailability after oral administration, inappropriate tissue localization and consequently poor therapeutic application.

OBJECTIVE

The present study investigates the complexation of AGP with HA to increase its solubility and hepatoprotective efficacy.

MATERIALS AND

METHODS

Complexes prepared by solvent evaporation in various weight ratios were characterized using differential scanning calorimetry, Fourier Transform InfraRed spectroscopy, X-ray diffraction, and scanning electron microscopy.

RESULTS AND DISCUSSION: The complexed AGP demonstrated improved solubility, dissolution, and permeation across rat intestine. It also displayed better hepatoprotection against carbontetrachloride-induced liver toxicity than the free drug in rats.

CONCLUSION

Complexation with HA is a valuable technique to improve solubility and bioavailability of pharmaceuticals.