The metabolism of a series of ester pro-drugs by NCTC 2544 cells, skin homogenate and LDE testskin

Lame, K.A., Denyer, S.P., Sanderson, .FD. and Shaw, P.N. (1994) The metabolism of a series of ester pro-drugs by NCTC 2544 cells, skin homogenate and LDE testskin. Journal of Pharmacy and Pharmacology, 46 12: 965-973.


Author Lame, K.A.
Denyer, S.P.
Sanderson, .FD.
Shaw, P.N.
Title The metabolism of a series of ester pro-drugs by NCTC 2544 cells, skin homogenate and LDE testskin
Journal name Journal of Pharmacy and Pharmacology   Check publisher's open access policy
ISSN 0022-3573
2042-7158
Publication date 1994-12
Sub-type Article (original research)
Volume 46
Issue 12
Start page 965
End page 973
Total pages 9
Place of publication West Sussex, United Kingdom
Publisher John Wiley & Sons
Language eng
Abstract The metabolism of a series of substituted pyrazolopyridine ester pro-drugs was investigated using NCTC 2544 cells, human skin homogenate and LDE Testskin as model systems. The compounds were incubated in each system and the disappearance of drug and the production of the major hydrolysis product was observed with time and quantitated using HPLC. The toxicity of the ester pro-drugs and the metabolites was examined in NCTC 2544 cells using a cell viability assay procedure. Hydrolytic activity was slightly higher in the cell culture model than in skin homogenate solution but the rank order of activity for each pro-drug was similar. The metabolic activity of LDE Testskin was much reduced compared with the other systems, but again the overall pattern of metabolism was not dissimilar. These findings indicate that NCTC 2544 cells provide a reasonable model for human skin ester hydrolysis both in terms of rate and in terms of substrate specificity.
Keyword Physical Model Evaluation
Topical Prodrug Delivery
Biological-membranes
Percutaneous-absorption
Simultaneous Transport
Enhanced Delivery
Dermal Delivery
Organ-culture
Invitro
Bioconversion
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ
Additional Notes Article first published online: 12 April 2011.

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Pharmacy Publications
 
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Created: Mon, 20 Dec 2010, 14:08:51 EST