Brinkmann I, Müller-Goymann C C
Institute of Pharmaceutical Technology, Technical University Braunschweig, Germany.
Pharmazie. 2005 Mar;60(3):215-20.
The present study is a comparison of the influences of glycerol, propylene glycol (PG), isopropyl myristate (IPM) and a combination of PG and IPM (1/1; w/w) on human stratum corneum (SC) by means of differential scanning calorimetry (DSC) and wide and small angle X-ray-diffraction (WAXD and SAXD). The effects of glycerol and PG on SC structure can be attributed to their functional groups. In DSC transition temperatures of lipid fractions are decreased whereas SAXD long distances of lamellar phases reveal an additional interference due to an integration into hydrophilic regions of hexagonally packed lipids (PG) or orthorhombically packed lipids (glycerol). The increased repeat distance is attributed to the polar character of both molecules. However, with IPM the long distance remains unaffected. IPM is integrated into the lipophilic regions of SC lipid matrix as concluded from an increase of WAXD reflections of orthorhombical lipids and a decrease of WAXD reflections of hexagonal lipids. The combination of PG/IPM affects SC microstructure in a specific manner. DSC shows a decrease in transition temperatures of the lipid fractions, although not as much as expected from the single substances. Additionally, the combination of IPM/PG affects the short distances of orthorhombically and hexagonally packed lipids in WAXD measurements similar as PG alone, whereas the long distance seems to remain unaffected as in the case of IPM pretreatment. Adjuvants with penetration enhancing potential reveal different effects on SC lipid microstructure, which have to be kept in mind in terms of formulating systems for transdermal administration.
本研究通过差示扫描量热法(DSC)以及广角和小角X射线衍射法(WAXD和SAXD),比较了甘油、丙二醇(PG)、肉豆蔻酸异丙酯(IPM)以及PG与IPM的组合(1/1;w/w)对人体角质层(SC)的影响。甘油和PG对SC结构的影响可归因于它们的官能团。在DSC中,脂质部分的转变温度降低,而SAXD中层状相的长间距显示出由于整合到六方堆积脂质(PG)或正交堆积脂质(甘油)的亲水区而产生的额外干涉。重复距离的增加归因于这两种分子的极性特征。然而,对于IPM,长间距不受影响。从正交脂质的WAXD反射增加和六方脂质的WAXD反射减少可以得出结论,IPM整合到SC脂质基质的亲脂区域中。PG/IPM的组合以特定方式影响SC微观结构。DSC显示脂质部分的转变温度降低,尽管不如单一物质预期的那么多。此外,在WAXD测量中,IPM/PG的组合对正交堆积和六方堆积脂质的短间距的影响与单独使用PG时相似,而长间距似乎像IPM预处理的情况一样不受影响。具有渗透增强潜力的佐剂对SC脂质微观结构显示出不同的影响,在制定透皮给药系统时必须牢记这一点。