Enhancing effect of polyoxyethylene alkyl ethers on the skin permeation of ibuprofen.
The influence of polyethoxylated non-ionic surfactants on the transport of ibuprofen across rat skin was investigated. The skin permeation of ibuprofen from a series of 17 polyoxyethylene (POE) alkyl ethers containing 5% ibuprofen was determined using Franz diffusion cells fitted with excised rat skins. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR) were performed for the physicochemical characterization of ibuprofen-surfactant interaction. In vitro transdermal flux through excised rat skin was found in the decreasing order of POE(5)cetyl/oleyl ether (110.24 microg/cm(2)/h)>POE(2)lauryl ether (99.91 microg/cm(2)/h)>POE(2)oleyl ether (67.46 microg/cm(2)/h)>POE(10)stearyl ether (66.19 microg/cm(2)/h). POE(2)oleyl ether showed the longest lag time (2.47 h). The enhancers containing the EO chain length of 2-5, HLB value of 7-9 and an alkyl chain length of C16-C18 were effective promoters of ibuprofen flux. FT-IR and DSC studies to probe the nature of the interaction between the ibuprofen and surfactant indicated that the hydrogen bonding state of ibuprofen was changed from the dimeric form to the carbonyl-hydroxyl (C=O-HO) hydrogen bond form in the presence of excess POE alkyl ether. These results indicated that this new system may be used in developing a transdermal formulation with improved skin permeation of ibuprofen.
Park
E S
ES
College of Pharmacy, Sungkyunkwan University, 440-746, Suwon, South Korea.
Chang
S Y
SY
Hahn
M
M
Chi
S C
SC
D000465:Algorithms; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D007052:Ibuprofen / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D014677:Pharmaceutical Vehicles; D011092:Polyethylene Glycols / Q000494:pharmacology*; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013268:Stimulation, Chemical; D013329:Structure-Activity Relationship; D013501:Surface-Active Agents / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D014677:Pharmaceutical Vehicles; D013501:Surface-Active Agents; D011092:Polyethylene Glycols; D007052:Ibuprofen