Preparation and evaluation of luteolin–phospholipid complex as an effective drug delivery tool against GalN/LPS induced liver damage

Abstract

Context: The phyto-phospholipid complexation technique is a promising approach to improve the bioavailability and efficacy of flavonoids.

Objective: The objective of this study was to improve the bioavailability and efficacy of luteolin by phospholipid complexation against inflammatory liver damage.

Materials and methods: The phospholipid complex of luteolin (LPC) was prepared by solvent evaporation accompanied by freeze drying. The physicochemical properties of LPC were investigated by means of spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD). Pharmacokinetic parameters in rats were determined and the hepatoprotective potential was assessed against d-galctosamine and lipopolysaccharide (GalN/LPS) induced hepatic damage.

Results: LPC showed drug loading of 74.14% and average particle size 147.4 nm. The results of FTIR, thermal and diffraction studies confirmed the formation of complex. The aqueous/n-octanol solubility showed improvements. LPC showed an increase in relative in vivo bioavailability to 535.31% of pure luteolin. The histological and biochemical changes induced by GalN/LPS were significantly ameliorated by LPC.

Discussion: Hepatoprotective effect of LPC was more profound than luteolin with a particle size suitable for passive targeting of inflammatory sites.

Conclusion: LPC was successfully formulated under optimized conditions and is an efficient drug delivery system for oral administration of luteolin with enhanced bioavailability and hepatoprotective potential.

• Bioavailability
• hepatoprotective
• luteolin
• phospholipid complex

Acknowledgements

The authors thank LIPOID, Germany for providing phospholipids as gift sample. The authors acknowledge Department of Science and Technology (No. SR/FST/LSI-434/2010), New Delhi (SERC Division), India for providing financial assistance under DSTFIST scheme as well as the Maulana Azad National Fellowship (MANF) UGC, New Delhi, India for providing financial assistance.

Declaration of interest

The authors report no conflict of interest. The authors alone are responsible for this work.