Synthesis and Performance of A Novel Penetration Enhancer

Abstract

Abstract-Preparation and percutaneous absorption of 2-methyl-2-perfluoro-2′-methyl-3′-oxoca-proyloxyl ethoxycarbonyl ethylmethyldipolyethoxylsilicane (V) were investigated. V was synthesized from 2-perfluoro-2′-methyl-3′-oxocaproyloxylethyl methacrylate and methyldichlorosilicane by hydrosilication, then by alcoholysis with polyglycol, and was characterized by FTIR and MS. The penetration percentage of diclofenac sodium in different solutions of 2% 1-menthol, 0.5% V, 2% 1-menthol-0.5% V and 2% azone were respectively determined with improved Franz equipment and using rat skin as transderma barrier. The enhancement ratios were 3.11, 1.19, 5.46 and 6.21, respectively. V with 1-menthol could improve the trasdermal amount of diclofenac sodium, especially, but sole V express bad performance for it.