Abstract
α-(4-(Diethoxyphosphorimidoyl)butyl)-oligodimethylsiloxane (ODMS-PHOS) was prepared from ODMS containing amino group at the chain end. The prepolymer was synthesized by a ring-opening polymerization of hexamethylcyclotrisiloxane (D3) initiated with lithium trimethylsilanolate, followed by a termination with 3-cyanopropyldimethylchlorosilane and a reduction of the cyano group with lithium alminium hydride. Its enhancing activity on the drug penetration through the skin was studied by in vitro experiment using 2-chamber diffusion cell. All the oligomers effectively enhanced the drug penetration and the permeation coefficients were 4–15 times as much as that without enhancer. The enhancing activity decreased with the increase of the average degree of polymerization. From the detailed analysis of the permeation profile, it was revealed that the partition of the drug from the vehicle to the skin considerably increased, however, diffusivity of the drug in the skin barrier was unchanged as compared with that without enhancer.
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