Effect of mucosal lipid components on the membrane permeation of water-soluble drugs.

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Abstract
The contribution of intestinal mucosal lipid components to the membrane permeation process of water-soluble drugs was examined by using liposomes as a model membrane. Mucosal lipids extracted from the rat small intestine were fractionated into several lipid classes by column chromatography and each lipid fraction was reconstituted into the liposomal membrane. The release rate of drugs incorporated in liposomes was measured (pH 6.5) as an index of the membrane permeability. 6-Carboxyfluorescein (6-CF), procainamide ethobromide (PAEB) and sulfanilic acid (SA) were employed as model drugs. Their absorption percentages from rat small intestine in 1 h were 2.4%, 3.2% and 7.5%, respectively, as determined by the in situ recirculation technique (pH 6.5). These drugs were more permeable through the liposomal membranes containing intestinal free fatty acids than egg lecithin liposomes, with the exception of SA. Arrhenius plots of the release rate constants indicated that increased liposomal membrane fluidity was partly responsible for this accelerated release in the case of PAEB, but no significant change was observed in the activation energy for the membrane permeation of 6-CF. Lipid components, especially free fatty acids of the intestinal mucosa, evidently play an important role in the absorption process of these water-soluble drugs.

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