Decrease in Skin Permeation and Antibacterial Effect of Parabens by a Polymeric Additive, Poly(2-methacryloyloxyethyl phosphorylcholine-co-butylmetacrylate)

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The inhibitory effect of poly(2-methacryloyloxyethyl phosphorylcholine-co-butylmetacrylate)(PMB) on the in vitro skin permeation of p-hydroxybenzoic acid and its esters (parabens ; methylparaben, ethylparaben, npropylparaben and n-butylparaben) as model compounds was evaluated. Solubility of the parabens in distilled water was increased by addition of PMB, and the increasing ratio was dependent on the concentration of PMB. The increment of the ratio was more marked in lipophilic parabens than hydrophilic ones. Skin permeability of parabens from their aqueous suspensions was decreased by addition of PMB, and the decreasing ratio was dependent on the PMB concentration. Then, antibacterial effect of parabens of their aqueous solutions was determined with and without PMB by measuring minimum inhibitory concentration (MIC) against E. coli and S. aureus. As results, MIC and antibacterial effect were increased and decreased, respectively, by addition of PMB. The contribution of PMB was more marked in butylparaben than methylparaben. These decreases in skin permeation and antibacterial effect of parabens by PMB are probably due to a higher solubility in water and a lower partition to the skin and bacterial membranes of parabens by addition of PMB.
公益社団法人日本薬学会の論文
2005-03-01