Untitled

Bucks, Daniel A. W.

doi:10.1023/a:1016340423079

Cited by 57 publications

(2 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The potential to use the metabolic activity of the skin to convert lipophilic prodrugs into more hydrophilic drugs was recognized by Bucks. 74 The approach to improve transdermal delivery with the use of prodrugs has been recently reviewed. 75…”

Section: Prodrugsmentioning

confidence: 99%

In VitroSkin Permeation Methodology

Finnin

Walters²,

Franz³

2011

Topical and Transdermal Drug Delivery

View full text Add to dashboard Cite

Section: Prodrugsmentioning

confidence: 99%

In VitroSkin Permeation Methodology

Finnin

Walters²,

Franz³

2011

Topical and Transdermal Drug Delivery

View full text Add to dashboard Cite

“…In addition, it can activate penetrating substances enzymatically by converting prodrugs to their active forms, catalyzed by specific metabolic enzymes present in the skin [ 7 ]. Understanding skin metabolism has become increasingly relevant in the design of prodrugs to target a specific site of action [ 8 ] in a drug discovery setting and safety assessment of consumers and drug products [ 9 ]. The activity of human skin enzymes has been described in various published reviews [ 9 , 10 ].…”

Section: Introductionmentioning

confidence: 99%

Human Skin Drug Metabolism: Relationships between Methyl Salicylate Metabolism and Esterase Activities in IVPT Skin Membranes

et al. 2023

View full text Add to dashboard Cite

The presence of esterase enzymes in human skin and their role in drug metabolism has been reported, but their distribution in the various skin layers and the relative contributions of those layers to metabolism is poorly defined. To gain further insight into esterase distribution, we performed in vitro skin permeation of a commercial 28.3% methyl salicylate (MeSA) cream (Metsal™) in Franz diffusion cells, using a range of human skin membranes, all from the same donor. The membranes were viable epidermis separated by a dispase II enzymatic method, heat separated epidermis, dermatomed skin, and dermis separated by a dispase II enzymatic method. Methyl salicylate and its metabolite, salicylic acid (SA), were measured by high-performance liquid chromatography. Alpha naphthyl acetate and Hematoxylin and Eosin staining provided qualitative estimations of esterase distribution in these membranes. The permeation of methyl salicylate after 24 h was similar across all membranes. Salicylic acid formation and permeation were found to be similar in dermatomed skin and dermis, suggesting dermal esterase activity. These results were supported by the staining studies, which showed strong esterase activity in the dermal–epidermal junction region of the dermis. In contrast with high staining of esterase activity in the stratum corneum and viable epidermis, minimal stained and functional esterase activity was found in heat-separated and dispase II-prepared epidermal membranes. The results are consistent with dispase II digesting hemidesmosomes, penetrating the epidermis, and affecting epidermal esterases but not those in the dermis. Accordingly, whilst the resulting dispase II-generated dermal membranes may be used for in vitro permeation tests (IVPT) involving esterase-based metabolic studies, the dispase II-generated epidermal membranes are not suitable for this purpose.

show abstract

Safety of Permethrin vs Lindane for the Treatment of Scabies

Meinking¹

1996

Arch Dermatol

View full text Add to dashboard Cite

Untitled

Cited by 57 publications

References 31 publications

In VitroSkin Permeation Methodology

In VitroSkin Permeation Methodology

Human Skin Drug Metabolism: Relationships between Methyl Salicylate Metabolism and Esterase Activities in IVPT Skin Membranes

Safety of Permethrin vs Lindane for the Treatment of Scabies

Contact Info

Product

Resources

About