Abstract

FORMULATION DEVELOPMENT AND EVALUATION OF ANTIOXIDANT POTENTIAL OF HESPERIDIN NANOCRYSTALS

Jibin Joy Varghese* and Rashmi Mallya

Abstract

Objective: The objective of this study was to prepare and investigate hesperidin nanocrystal and investigate its antioxidant potential. Materials and Methods: Nanosuspensions of hesperidin were prepared by NANOEDGE™ method using optimized combination of HPMC E5 and Poloxamer 188 as stabilizers. The nanosuspension was spray dried to obtain solid dry nanocrytals of hesperidin and formulated into capsules and evaluated. Results: The nanosuspensions of hesperidin were successfully prepared. The concentrations of different stabilizers influenced the particle size of nanosuspensions. Spray drying of nanosuspension resulted in free flowing nanocrystals. Spray dried nanocrystal were needle shaped. The X-ray powdered diffraction and differential scanning calorimetry results indicated that there was no change in the crystalline nature of hesperidin. Hesperidin nanocrystals increased the saturation solubility to an extent of 5-times. Capsules incorporating hesperidin nanocrystal dissolved 5 times more as compared to pure hesperidin capsules. In-vitro antioxidant studies carried out on hesperdin nanocrystals showed that it has antioxidant potential as comparable to pure hesperdin. In-vivo studies on carbon tetrachloride induced liver toxicity studies on rat confirmed significant antioxidant potential of hesperidin nanocrystals at a dose of 50 mg/kg compared to pure hesperidin. Conclusions: Dissolution studies contended the ability of dried hesperidin nanocrystals to enhance dissolution rate of the drug compared to its crude form. Furthermore, dried hesperidin nanocrystals could significantly improve and retain the antioxidant potential of hesperidin.

Keywords: Hesperidin, NANOEDGEâ„¢, nanocrystals, liver toxicity, in vivo antioxidant.