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Predicting topical drug clearance from the skin

Authors :
Annette L. Bunge
M. Begoña Delgado-Charro
Richard H. Guy
Magdalena Hoppel
Maria Alice Maciel Tabosa
Source :
Drug Delivery and Translational Research
Publication Year :
2020
Publisher :
Springer Science and Business Media LLC, 2020.

Abstract

For topical drug products that target sites of action in the viable epidermal and/or upper dermal compartment of the skin, the local concentration profiles have proven difficult to quantify because drug clearance from the viable cutaneous tissue is not well characterised. Without such knowledge, of course, it is difficult—if not impossible—to predict a priori whether and over what time frame a topical formulation will permit an effective concentration of drug within the skin ‘compartment’ to be achieved. Here, we test the hypothesis that valuable information about drug disposition, and specifically its clearance, in this experimentally difficult-to-access compartment (at least, in vivo) can be derived from available systemic pharmacokinetic data for drugs administered via transdermal delivery systems. A multiple regression analysis was undertaken to determine the best-fit empirical correlation relating clearance from the skin to known or easily calculable drug properties. It was possible, in this way, to demonstrate a clear relationship between drug clearance from the skin and key physical chemical properties of the drug (molecular weight, log P and topological polar surface area). It was further demonstrated that values predicted by the model correlated well with those derived from in vitro skin experiments.

Details

ISSN :
21903948 and 2190393X
Volume :
11
Database :
OpenAIRE
Journal :
Drug Delivery and Translational Research
Accession number :
edsair.doi.dedup.....9bb2747d9a5a56d054505e960de1d3ea
Full Text :
https://doi.org/10.1007/s13346-020-00864-8