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• W2023985001 abstract "Abstract 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 duodenum mucosal sites. The transport of rhEGF across the gastrointestinal mucosa was investigated using [125I]rhEGF. Possibly due to the strong barrier function of the membrane, the transported amount of [125I]rhEGF across the intestinal mucosa was less than 3% up to 3 h. Moreover, the unlabeled rhEGF (16.7 or 50 μg/ml) had no significant effect on the tracer (0.29 μCi/ml rhEGF) penetration. Effects of various additives on the penetration of rhEGF across the colon were then investigated. Glyceryl palmitostearate, sodium caprate, sodium lauryl sulfate and Tween 80 had no significant effect on the [125I]rhEGF penetration across the colon. Thus, low penetration of rhEGF with or without various additives might be responsible for the barrier function of the membrane rather than the enzymatic degradation." @default.
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• W2023985001 title "Site-specific degradation and transport of recombinant human epidermal growth factor (rhEGF) in the rat gastrointestinal mucosa" @default.
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• W2023985001 doi "https://doi.org/10.1016/s0378-5173(98)00097-0" @default.
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