Decrease in skin permeation and antibacterial effect of parabens by a polymeric additive, poly(2-methacryloyloxyethyl phosphorylcholine-co-butylmetacrylate).
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.
Hasegawa
Tetsuya
T
Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan.
Kim
Soan
S
Tsuchida
Mamoru
M
Issiki
Yasunori
Y
Kondo
Seiichi
S
Sugibayashi
Kenji
K
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
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)