カプロイルリゾチームの合成とラットにおけるリンパ移行性の改善

概要

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Lysozyme(Mw : 14, 300) was derivatized by chemical modification with caproic anhydride to the N-terminal of lysine residue. The product observed to be more lipophilic than parent lysozyme by high-performance liquid chromatography. The activity and modified percentage of amino groups of caproyl derivative were 76.5% and 40% of parent lysozyme, respectively. Intestinal absorption of lysozyme and caproyl derivative was examined by <I>in situ</I> closed small intestinal loops of rats. A significant increase in cumulative amount of lymph fluid of caproyl derivative was found in comparison with that of parent lysozyme. However both compounds were not detected in plasma. Lysozyme and caproyl derivative were observed to be almost stable in phosphate buffered saline or lymph fluid <I>in vitro</I>. These findings suggested that acylation of lysozyme such as caproylation might be a useful approach for improving the lymphatic transport of enzyme with high molecular weight.
日本DDS学会の論文