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Topical Delivery of a Naproxen-Dithranol Co-drug: In Vitro Skin Penetration, Permeation, and Staining

Lookup NU author(s): Dr Wing Man LauORCiD

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Abstract

PurposeThis work probed the topical delivery and skin-staining properties of a novel co-drug, naproxyl-dithranol (Nap-DTH), which comprises anti-inflammatory (naproxen) and anti-proliferative (dithranol) moieties.MethodFreshly excised, full-thickness porcine ear skin was dosed with saturated solutions of the compounds. After 24 h, the skin was recovered and used to prepare comparative depth profiles by the tape-stripping technique and to examine the extent of skin staining.ResultsDepth profiles showed that Nap-DTH led to a 5-fold increase in drug retention in the skin compared to dithranol. The application of Nap-DTH also demonstrated improved stability, resulting in lower levels of dithranol degradation products in the skin. Furthermore, significantly less naproxen from hydrolysed Nap-DTH permeated into the receptor phase compared to naproxen when applied alone (0.08 ± 0.03 nmol cm^-² and 180 ± 60 nmol cm^-², respectively). Moreover, the reduced staining of the skin was very apparent for Nap-DTH compared to dithranol.ConclusionsTopical delivery of Nap-DTH not only improves the delivery of naproxen and dithranol, but also reduces unwanted effects of the parent moieties, in particular the skin staining, which is a major issue concerning the use of dithranol.

Publication metadata

Author(s): Lau WM, White AW, Heard CH

Publication type: Article

Publication status: Published

Journal: Pharmaceutical Research

Year: 2010

Volume: 27

Issue: 12

Pages: 2734-2742

Print publication date: 01/12/2010

Online publication date: 25/09/2010

ISSN (print): 0724-8741

ISSN (electronic): 1573-904X

Publisher: Springer

URL: https://doi.org/10.1007/s11095-010-0274-8

DOI: 10.1007/s11095-010-0274-8

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