Biopharmaceutic and Pharmacokinetic Evaluation of Hesperidin and Hesperetin for Ocular Delivery
type: CreativeWork
description: The bioflavonoid hesperidin and its aglycone hesperetin are promising candidates for the treatment of diabetic retinopathy and diabetic macular edema because of their pharmacological properties. The objective of this project was to characterize the biopharmaceutic and pharmacokinetic characteristics of hesperidin and hesperetin for ocular delivery, especially with respect to the distribution of these compounds to the posterior segment of the eye. Hesperidin and hesperetin were found to be water insoluble compounds. Although they demonstrated good permeability across the ocular tissues, hesperetin's permeability was found to be higher than that of hesperidin. Hesperidin demonstrated symmetrical transcorneal and transretinal permeation whereas hesperetin exhibited asymmetrical transcorneal and symmetrical transretinal transport. However, none of the influx or efflux transporters, expressed on the cornea, were involved in hesperetin's corneal transport. It was concluded that hesperetin's physicochemical properties, ultrastructure of the cornea and components of the diffusion media play a major role in the passive asymmetric transport. Results from the intravitreal kinetic studies of hesperidin, hesperetin and glucosyl-hesperidin (a water soluble derivative of hesperidin), following intravitreal injection, revealed that all three compounds have relatively short half-lives (< 8h) in the vitreous humor. Hesperetin demonstrated the shortest half-life, consistent with its physiochemical characteristics. All three compounds exhibited linear pharmacokinetics, within the dose range tested. This information will be critical in the design of ocular drug delivery systems for these compounds. The ocular bioavailability studies following systemic administration suggested that vitreal bioavailability is negligible because of rapid conversion of both hesperidin and hesperetin into their hydrophilic metabolite, hesperetin-glucuronide, in the plasma. In contrast, topical instillation p…
abstract: The bioflavonoid hesperidin and its aglycone hesperetin are promising candidates for the treatment of diabetic retinopathy and diabetic macular edema because of their pharmacological properties. The objective of this project was to characterize the biopharmaceutic and pharmacokinetic characteristics of hesperidin and hesperetin for ocular delivery, especially with respect to the distribution of these compounds to the posterior segment of the eye. Hesperidin and hesperetin were found to be water insoluble compounds. Although they demonstrated good permeability across the ocular tissues, hesperetin's permeability was found to be higher than that of hesperidin. Hesperidin demonstrated symmetrical transcorneal and transretinal permeation whereas hesperetin exhibited asymmetrical transcorneal and symmetrical transretinal transport. However, none of the influx or efflux transporters, expressed on the cornea, were involved in hesperetin's corneal transport. It was concluded that hesperetin's physicochemical properties, ultrastructure of the cornea and components of the diffusion media play a major role in the passive asymmetric transport. Results from the intravitreal kinetic studies of hesperidin, hesperetin and glucosyl-hesperidin (a water soluble derivative of hesperidin), following intravitreal injection, revealed that all three compounds have relatively short half-lives (< 8h) in the vitreous humor. Hesperetin demonstrated the shortest half-life, consistent with its physiochemical characteristics. All three compounds exhibited linear pharmacokinetics, within the dose range tested. This information will be critical in the design of ocular drug delivery systems for these compounds. The ocular bioavailability studies following systemic administration suggested that vitreal bioavailability is negligible because of rapid conversion of both hesperidin and hesperetin into their hydrophilic metabolite, hesperetin-glucuronide, in the plasma. In contrast, topical instillation p…
author: Srirangam, Ramesh
keywords: Biopharmaceutic, Delivery, Hesperetin, Hesperidin, Ocular, Pharmacokinetics, Pharmacy and Pharmaceutical Sciences
date published: 2011-01-01T08:00:00Z
date modified: 2026-07-24T03:05:22Z
provider: University of Mississippi
publisher: Networked Digital Library of Theses and Dissertations
type: WebPage
source organization: University of Mississippi