PMID: 8961171Nov 1, 1996Paper

Transport and metabolic pathway of thymocartin (TP4) in excised bovine nasal mucosa

The Journal of Pharmacy and Pharmacology
S LangH P Merkle

Abstract

Thymocartin (TP4, Arg-Lys-Asp-Val) is the 32-35 fragment of the naturally occurring thymic factor (thymopoietin). Here studies on the nasal transport and metabolism of TP4 were performed. Freshly excised bovine nasal mucosa was taken as a model membrane. For permeation studies typical donor-receiver experiments (side-by-side) and finite-dose experiments with small volumes of highly concentrated solutions were carried out. The metabolic pathway of TP4 in nasal mucosa was found to occur according to a typical aminopeptidase cleavage pattern, stepwise forming Lys-Asp-Val and Asp-Val. TP4 metabolism experiments under reflection kinetics showed a saturation profile above 0.5 mumol mL-1. A non-linear kinetic model consisting of three steps in sequence was sufficient to describe the kinetics: for the first step saturable Michaelis-Meat kinetics, and for the second and the third step first-order kinetics were assured. The model was capable of simultaneously fitting the data for the full range of initial concentrations from 0.1 up to 1.0 mumol mL-1. Saturation kinetics was also found to be the prominent feature of the permeation experiments performed. In the lower concentration range (< 0.4 mumol mL-1), transport of TP4 across nasal muc...Continue Reading

Citations

Jun 6, 2000·Advanced Drug Delivery Reviews·H P MerkleM C Schmidt
Dec 10, 1998·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·C WadellO Camber
Jan 28, 2003·Drug Discovery Today·Priyanka AroraSanjay Garg
Oct 10, 2006·AAPS PharmSciTech·Rita J MajithiyaRayasa S R Murthy
Oct 14, 2008·AAPS PharmSciTech·Grace RathnamR Ilavarasan
Dec 29, 2006·Drug Development and Industrial Pharmacy·Alexander GreimelMauro D'Antonio
Jun 19, 2007·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Elisabetta GaviniPaolo Giunchedi
Oct 28, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Preeti PandeyHarendra S Parekh
Sep 4, 2018·Expert Opinion on Drug Delivery·Wisam Al BakriZhen Yang

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