Dissolution Enhancement of Lycopene Compacts by Liquisolid Technique.

Abstract

Objectives: Lycopene is a powerful antioxidant with diverse health benefits. However, it belongs to the Biopharmaceutics Classification System II; thus, it depicts poor water solubility and dissolution. Its lipophilic nature hinders the bioavailability of this drug. To overcome these limitations, namely, poor solubility and bioavailability, several approaches have been tried so far, such as co-solvency, size reduction or micronization, complexation, adsorption on high surface area carriers, etc. The present research aimed to apply the liquisolid technique to prepare lycopene liquisolid compacts with an improved dissolution profile. The impact of parameters such as carrier and drug concentration percentage on drug dissolution was evaluated in liquisolid compacts.

Materials and methods: Lycopene was extracted by Soxhlet extractionand then characterized by ultraviolet spectroscopy, infrared spectroscopy, thin-layer chromatography, and melting point. Liquisolid compacts of lycopene were formulated by using excipients such as non-volatile solvent (glycerine), carrier (Avicel PH 101, Fujicalin, Neusilin US2), disintegrant (Croscarmellose sodium), and diluent (lactose). The different formulation batches of liquisolid compacts were formulated and evaluated based on different pre-compression and post-compression parameters.

Results: Powder X-ray Diffraction (PXRD) and Fourier transform infrared spectroscopy were utilized to analyze drug-excipient interaction; these studies showed no evidence of any physical or chemical interaction between the drug(s) and the excipients. The PXRD of lycopene showed sharp and intense peaks at diffraction angles (2θ) such as 12.563, 19.176, 19.636, 20.062, 21.283, 26.629, 29.479, 30.235, and 39.997, which indicates a crystallinestructure. The PXRD of the physical mixture of lycopene and excipients showed similar sharp peaks (12.582, 19.202, 19.634, 20.045, 21.304, 26.565, 29.474, 30.250, and 40.065), indicating thatthere is no drug-excipient interaction occurring. Lycopene was extracted and characterized. IR spectroscopy and PXRD showed no drug-excipient interaction. The lycopene liquisolid compacts passed both pre-compression and post-compression evaluations within acceptable limits.

Conclusion: The formulation batch F-7, formulated with Neusilin US2 as a carrier and 40% drug concentrationshowed 98% in vitro drug release and thus it was selected as the optimized formulation with improved dissolution.