Department of Clinical Pharmaceutics, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Department of Research, Nagoya Industrial Science Research Institute, 1-13 Yotsuyadori, Chikusa-ku, Nagoya 464-0819, Japan.
Int J Pharm. 2017 Apr 15;521(1-2):222-231. doi: 10.1016/j.ijpharm.2017.02.049. Epub 2017 Feb 21.
We evaluated the interaction between human stratum corneum (SC) and surfactant-based rigid or elastic vesicles during permeation using synchrotron X-ray diffraction to obtain the mechanism action of surfactant-based vesicles for enhanced skin permeation. The effects of vesicle elasticity on the interaction with SC were also investigated. Changes in the small-angle X-ray diffraction peaks of the human SC after buffer control and vesicle application were monitored. In the small-angle region, the control as the citrate buffer induced no significant changes of diffraction peaks for the lamellar structure of short periodicity phase (SPP), which is observed as a main peak in the human SC. Application of rigid vesicles resulted in small changes in the diffraction peaks attributed to lamellar phase of SPP. After application of elastic vesicles, however, a large shift to smaller angles due to swelling of the lamellar phase of SPP was clearly observed from the intensity difference profiles. All peaks due to the vesicles were still observed after 2h of application for all formulations, indicating that both vesicles interacted with the SC while maintaining their structures. These results strongly suggest that vesicles affect the lamellar phase of SPP of the intercellular lipids in the SC during permeation.
我们使用同步加速器 X 射线衍射评估了在渗透过程中人类角质层 (SC) 与基于表面活性剂的刚性或弹性囊泡之间的相互作用,以获得基于表面活性剂的囊泡增强皮肤渗透的机制作用。还研究了囊泡弹性对与 SC 相互作用的影响。监测了缓冲液对照和囊泡应用后人体 SC 小角度 X 射线衍射峰的变化。在小角度区域,作为对照的柠檬酸盐缓冲液不会引起短周期相 (SPP) 的层状结构的衍射峰发生显著变化,SPP 是人体 SC 中的主要峰。刚性囊泡的应用导致 SPP 的层状相的衍射峰发生微小变化。然而,在应用弹性囊泡后,由于 SPP 的层状相的肿胀,从强度差谱中清楚地观察到小角度的明显偏移。对于所有配方,在应用 2 小时后仍观察到所有囊泡的所有峰,表明所有囊泡都在与 SC 相互作用的同时保持其结构。这些结果强烈表明,囊泡在渗透过程中会影响 SC 中细胞间脂质的 SPP 的层状相。