Brinkmann I, Müller-Goymann C C
Institut für Pharmazeutische Technologie, Technische Universität Carolo-Wilhelmina zu Braunschweig, Braunschweig, Germany.
Skin Pharmacol Appl Skin Physiol. 2003 Nov-Dec;16(6):393-404. doi: 10.1159/000072935.
The influence of isopropyl myristate (IPM), isopropyl alcohol (IPA) and a combination of both was studied in view of hydrocortisone (HC) permeation across the human stratum corneum (SC). IPM, IPA and their combination were incorporated into water-containing hydrophilic ointment (WHS), and the resulting effects on HC permeation and on HC accumulation in human SC were investigated as well as the influence of these substances on the microstructure of the SC. Differential scanning calorimetry as well as wide- and small-angle X-ray diffraction show that IPM incorporation into SC results in densely packed bilayer lipids and a loss of order of the corneocyte-bonded lipids. Both effects result in a decreased diffusion coefficient of HC in SC and thus in a decreased permeation rate compared to that of HC from WHS. On the other hand, IPA fluidizes and disrupts the bilayer structure of the intercellular lipids. These effects, concomitant with an increased amount of dissolved HC within the ointment, increase the permeation rate of HC across SC. The combination of both ingredients effects a stronger fluidization and disruption of intercellular lipids than with IPA alone. Therefore, the permeation rate of HC across SC is higher than with IPA alone. Consequently, the IPM and IPA combination acts synergistically on the microstructure of SC.
研究了肉豆蔻酸异丙酯（IPM）、异丙醇（IPA）及其组合对氢化可的松（HC）透过人体角质层（SC）的影响。将IPM、IPA及其组合加入到含水亲水性软膏（WHS）中，研究其对HC透过人体SC以及在人体SC中蓄积的影响，以及这些物质对SC微观结构的影响。差示扫描量热法以及广角和小角X射线衍射表明，将IPM加入到SC中会导致双层脂质紧密堆积，且角质形成细胞结合脂质的有序性丧失。这两种效应都会导致HC在SC中的扩散系数降低，因此与来自WHS的HC相比，渗透速率降低。另一方面，IPA使细胞间脂质的双层结构流化并破坏。这些效应，再加上软膏中溶解的HC量增加，提高了HC透过SC的速率。两种成分的组合比单独使用IPA对细胞间脂质的流化和破坏作用更强。因此，HC透过SC的速率高于单独使用IPA时。因此，IPM和IPA组合对SC的微观结构具有协同作用。
