Evaluation of Nitrosyl Ruthenium Complexes Entrapped in an Oil-In- Water Emulsion as Vasodilator Agents

摘要

Several attempts have been made toward the production of oxide (NO)- releasing agents based on metalliccomplexes. However, many of these agents have been shown to undergo hydroxide electrophilic attack, thus generatingthe corresponding nitro species. Entrapped nitrosyl ruthenium species can be stabilized in an oil-in-water (o/w) emulsionand be further used for local NO delivery. This study describes the transdermal permeation of cis and trans-[RuCl(bpy)2NO](PF6)2 complexes as NO-donor agents from a topically applied emulsion, with NO release rates of 0.042± 0.002 and 0.035 ± 0.003 mol/cm2.h, respectively. In vitro skin permeation studies performed with the cis and trans-[RuCl(bpy)2(NO)](PF6)2 complexes in o/w emulsion showed that they tend to accumulate in the stratum corneum (SC)and viable skin, with spontaneous NO release occurring in the viable skin only. NO release was detected by using an NOsensorwhen the complexes were in contact with the sonicated skin. The vascular responses to the NO released from thecis and trans-[RuCl(bpy)2(NO)](PF6)2 complexes in o/w emulsion were also evaluated by vasodilation experiments.