Topical delivery of a naproxen-dithranol co-drug: in vitro skin penetration, permeation, and staining

Lau, Wing Man ORCID: https://orcid.org/0000-0002-2998-6470, White, Alex William ORCID: https://orcid.org/0000-0002-1539-0158 and Heard, Charles Martin ORCID: https://orcid.org/0000-0001-9703-9777 2010. Topical delivery of a naproxen-dithranol co-drug: in vitro skin penetration, permeation, and staining. Pharmaceutical Research 27 (12) , pp. 2734-2742. 10.1007/s11095-010-0274-8

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Abstract

Purpose: This 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. Method: Freshly 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. Results: Depth 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. Conclusions: Topical 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.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Pharmacy
Subjects:	R Medicine > RS Pharmacy and materia medica
Publisher:	Springer
ISSN:	0724-8741
Last Modified:	25 Oct 2022 09:59
URI:	https://orca.cardiff.ac.uk/id/eprint/60723

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