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Topical Delivery of a Naproxen-Dithranol Co-drug: In Vitro Skin Penetration, Permeation, and Staining
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Topical Delivery of a Naproxen-Dithranol Co-drug: In Vitro Skin Penetration, Permeation, and Staining
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Journal Article
Topical Delivery of a Naproxen-Dithranol Co-drug: In Vitro Skin Penetration, Permeation, and Staining
2010
Overview
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.
Publisher
Boston : Springer US,Springer US,Springer,Springer Nature B.V
Subject
/ Animals
/ Anthralin - administration & dosage
/ Anthralin - pharmacokinetics
/ Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
/ Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
/ Biological and medical sciences
/ Biomedical and Life Sciences
/ Biomedical Engineering and Bioengineering
/ Chromatography, High Pressure Liquid
/ co-drug
/ Dermatologic Agents - administration & dosage
/ Dermatologic Agents - pharmacokinetics
/ Naproxen - administration & dosage
/ Nonsteroidal anti-inflammatory drugs
/ Pharmaceutical technology. Pharmaceutical industry
/ Pharmacology. Drug treatments
/ Pharmacy
/ prodrug
/ Skin
/ Swine
