Vaishali Anil Kilor, Nidhi P. Sapkal, Gunjan V. Vaidya

Gurunanak College of Pharmacy, Nari, Kamgaar Nagar, Kamptee Road, Nagpur, India

Abstract:

Bioflavonoid hesperidin is used primarily to assist treatment of capillary disorders like hemorrhoids and varicose veins, by reducing capillary permeability. There are certain limitations to the use of these bioflavonoids in the pharmaceutical formulations because of their physical properties like limited aqueous solubility, poor bioavailability and high oral dose. Therefore in the present research work microemulsions of hesperidine were developed for improving solubility and bioavailability using topical route. These microemulsions were then converted into ointment for ease of application. Optimized o/w microemulsion of hesperidin composed of eucalyptus oil 20%, Tween-80/Acconon CC-6(2:1) 33% and water. It was observed from ex vivo permeation studies that flux value for optimized microemulsion was found to be 8.971µg/ml/cm2 as compared to pure hesperidin (1.230 µg/ml/cm2). This formulation was then converted into ointment by using optimized base containing PEG-6000, PEG-400 and Cetyl alcohol. This microemulsion based ointment passed all the characterization tests (droplet size analysis using PCS, ex vivo permeation studies, in vivo bioavailability studies etc.) as well as remained stable for the period of 3 months during stability studies as per ICH guidelines. The bioavailability studies of hesperidin microemulsion based ointment in rats showed 3 fold statistically significant (p<0.001) improvement in bioavailability as compared to microemulsion when applied topically. Thus it can be concluded that components of microemulsion and ointment are contributing to improve bioavailability of hesperidin.