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Site-specific degradation and transport of recombinant human epidermal growth factor (rhEGF) in the rat gastrointestinal mucosa by Kun Han; Myoung Sille Choi; Youn Bok Chung is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

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The purpose of the present study was to elucidate the site specificity of degradation of recombinant human epidermal growth factor (rhEGF) in the gastrointestinal mucosa and to screen absorption enhancers and enzyme inhibitors for the development of an rhEGF oral delivery system. The degradation of rhEGF after incubation with the rat mucosal sites was determined by measuring the disappearance of rhEGF as well as the appearance of metabolites by HPLC. Two degradation products of rhEGF, M-I and M-II, were detected. Comparing peak appearance order of rhEGF and its metabolites with the previous reports, M-I and M-II were estimated to be products by oxidation at the methionine residue, and by deamidation at the asparagine residue, respectively. The rhEGF degradation order was duodenum \ileum\stomach\ jejunum \ colon. rhEGF was rapidly degraded in the duodenum and the ileum, while relatively stable in the colon and jejunum mucosal sites. Sodium caprate slightly inhibited the rhEGF degradation, whereas STDHF or EDTA had no effect on its degradation in the jejunum mucosal sites. The degradation of rhEGF was inhibited by the addition of bestatin, sodium caprate or sodium salicylate in the d

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Author

Kun Han; Myoung Sille Choi; Youn Bok Chung

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0378-5173)

Published

1998

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)