Passive asymmetric transport of hesperetin across isolated rabbit cornea.

Abstract:

:Hesperetin, an aglycone of the flavanone hesperidin, is a potential candidate for the treatment of diabetic retinopathy and macular edema. The purpose of this investigation was to determine solubility, stability and in vitro permeability characteristics of hesperetin across excised rabbit corneas. Aqueous and pH dependent solubility was determined using standard shake flask method. Solution stability was evaluated as a function of pH (1.2-9) and temperature (25 and 40 degrees C). Permeability of hesperetin was determined across the isolated rabbit cornea utilizing a side-bi-side diffusion apparatus, in the apical to basolateral (A-B) and basolateral to apical (B-A) directions. Hesperetin displayed asymmetrical transcorneal transport with a 2.3-fold higher apparent permeability in the B-A direction compared to the A-B direction. The transport process was observed to be pH dependent. Surprisingly, however, the involvement of efflux transporters or proton-coupled carrier-systems was not evident in this asymmetric transcorneal diffusion process. The passive and pH dependent corneal transport of hesperetin could probably be attributable to corneal ultrastructure, physicochemical characteristics of hesperetin and the role of transport buffer components.

journal_name

Int J Pharm

authors

Srirangam R,Majumdar S

doi

10.1016/j.ijpharm.2010.04.036

subject

Has Abstract

pub_date

2010-07-15 00:00:00

pages

60-7

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(10)00308-X

journal_volume

394

pub_type

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