title: Decrease in skin permeation and antibacterial effect of parabens by a polymeric additive, poly(2-methacryloyloxyethyl phosphorylcholine-co-butylmetacrylate).
abstract: 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, n-propylparaben 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.
authors.affiliation: Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan.
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Hasegawa
authors.forename: Soan
authors.initials: S
authors.lastname: Kim
authors.forename: Mamoru
authors.initials: M
authors.lastname: Tsuchida
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Issiki
authors.forename: Seiichi
authors.initials: S
authors.lastname: Kondo
authors.forename: Kenji
authors.initials: K
authors.lastname: Sugibayashi
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000378:metabolism / Q000493:pharmacokinetics* / Q000494:pharmacology; D000891:Anti-Infective Agents, Local / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D004058:Diffusion; D008689:Methacrylates / Q000737:chemistry / Q000494:pharmacology*; D010226:Parabens / Q000378:metabolism / Q000493:pharmacokinetics* / Q000494:pharmacology; D010539:Permeability; D010767:Phosphorylcholine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D011108:Polymers / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D012867:Skin / Q000378:metabolism*; D012996:Solutions / Q000737:chemistry; D014867:Water / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D000891:Anti-Infective Agents, Local; D008689:Methacrylates; D010226:Parabens; D011108:Polymers; D012996:Solutions; D014867:Water; D010767:Phosphorylcholine; C079200:poly(2-methacryloyloxyethyl phosphorylcholine-co-n-butyl methacrylate)