Park E S, Chang S Y, Hahn M, Chi S C
College of Pharmacy, Sungkyunkwan University, 440-746, Suwon, South Korea.
Int J Pharm. 2000 Nov 19;209(1-2):109-19. doi: 10.1016/s0378-5173(00)00559-7.
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.
研究了聚乙氧基化非离子表面活性剂对布洛芬透过大鼠皮肤转运的影响。使用装有切除大鼠皮肤的Franz扩散池,测定了含5%布洛芬的17种聚氧乙烯(POE)烷基醚系列中布洛芬的皮肤渗透情况。采用差示扫描量热法(DSC)和傅里叶变换红外光谱法(FT-IR)对布洛芬-表面活性剂相互作用进行了物理化学表征。发现体外透过切除大鼠皮肤的透皮通量顺序为:POE(5)十六烷基/油基醚(110.24μg/cm²/h)>POE(2)月桂基醚(99.91μg/cm²/h)>POE(2)油基醚(67.46μg/cm²/h)>POE(10)硬脂基醚(66.19μg/cm²/h)。POE(2)油基醚的滞后时间最长(2.47小时)。含有2-5个EO链长、7-9的HLB值和C16-C18烷基链长的增强剂是布洛芬通量的有效促进剂。FT-IR和DSC研究以探究布洛芬与表面活性剂之间相互作用的性质,结果表明在过量POE烷基醚存在下,布洛芬的氢键状态从二聚体形式转变为羰基-羟基(C=O-HO)氢键形式。这些结果表明,该新体系可用于开发一种改善布洛芬皮肤渗透性的透皮制剂。