Novel transdermal drug penetration enhancer: synthesis and enhancing effect of alkyldisiloxane compounds containing glucopyranosyl group

摘要: Abstract The syntheses of alkyldisiloxanes containing sugar moiety with various alkyl chain length were investigated, in order to develop a silicone-based transdermal penetration enhancer which was expected show low irritation the skin. 1-Alkyl-3-β- d -glucopyranosyl-1,1,3,3-tetramethyldisiloxanes (Glc–SiCs) prepared by two-step hydrosilylations 1-alkene and 1-allyl-β- -glucose tetraacetate 1,1,3,3-tetramethyldisiloxane presence bis(benzonitrile)platinum dichloride as catalyst, followed hydrolysis acetyl groups sodium methoxide. enhancing effect Glc–SiCs on percutaneous drug evaluated vitro experiments using two-chamber diffusion cell. Antipyrine (ANP) indomethacin (IND) used hydrophilic hydrophobic model drugs, respectively, amount permeating through rat abdominal skin or without estimated HPLC. As result, exhibited permeation both drugs skin, influenced Glc–SiCs. In addition, it suggested that suitable balance polarity would be necessary appear high effect, where octyl decyl highest effect. From determination kinetic parameters permeation, also found this due increase partition coefficients By determine cholesterol extracted from defatting one functions resulted activity. Furthermore, according Draize test, confirmed showed