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A literature data set of 112 corneal permeability measurements was analysed, to determine whether mechanistically based structure-permeability relationships (SPRs) could be developed for the transport of structurally diverse chemicals across the rabbit cornea.

Four physicochemical properties were found to be statistically significant: the logarithm of the octanol-water partition coefficient (logP), molecular weight (MW), the third-order kappa index [k3]), and the hydrogen-bonding capacity (nH), which provide measures of lipophilicity , molecular size, molecular shape, and hydrogen-bonding capacity , respectively. In particular, a two-variable SPR, based on logP and MW, and a three-variable SPR, based logP, k3 and nH, were found to be statistically-significant (p<0.001) and to have stable coefficients. SPRs such as these could be used during the drug discovery process as a first step in the prediction of transcorneal delivery.

Additional information

Authors: WORTH A, EVCAM, Institute for Health and Consumer Protection, Joint Research Centre, European Commission, 21020 Ispra (IT);CRONIN T, School of Pharmacy and Chemistry, Liverpool John Moores University, Byrom Street, Liverpool L3 3AF (UK)
Bibliographic Reference: Article: Alternatives to Laboratory Animals (ATLA) 28, (2000), pp. 403-413
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