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Current Drug Therapy

Author(s): Bhupen Kalita* and Bhargab Nath Patwary

DOI: 10.2174/1574885514666190226155933

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Formulation and in vitro Evaluation of Hesperidin-Phospholipid Complex and its Antioxidant Potential

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Abstract

Background: The recent trend of herbal drug delivery has been focused on developing novel drug delivery carriers to address problems related to solubility, oral bioavailability, skin permeation and stability. The phyto-phospholipid complex (phytosomes®) technology has been used to overcome the problems associated with many conventional herbal extracts.

Aim: The present work aimed to formulate phospholipid-complex of the flavanoid Hesperidin to enhance its dissolution leading to enhanced oral bioavailability.

Method: The complex was prepared by refluxing various molar ratios of hesperidin and PC followed by solvent evaporation. The prepared complexes were evaluated for saturation solubility, partition co-efficient and drug content. The free drug and phospholipid complexes were analyzed in DSC. Surface morphology of the prepared complexes was viewed using SEM images. Selected formulations were subjected to in vitro drug release study. Antioxidant effect was examined by free radical scavenging method.

Results: Solubility and partition coefficient of the prepared complexes were improved in comparison to free drug. Based on the results of solubility, partition coefficient and drug content, formulation F2 was selected as an optimized batch. DSC thermograms confirmed the formation of phospholipid complex. Free Hesperidin and Hesperidin-phospholipid complex (F2) showed 46.9 % and 78.20 % of drug release, respectively, at seven hours phosphate buffer (pH 7.4). The optimized formulation showed concentration-dependent anti-oxidant property.

Conclusion: Results of the present study suggested that the phospholipid complex of Hesperidin possesses the antioxidant potential and may be of potential use for improving the dissolution of hesperidin and hence oral bioavailability.

Keywords: Hesperidin, phospholipid complex, phytosomes, herbosomes, solubility, antioxidant.

Graphical Abstract

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