Study on the drug permeation mechanism from flurbiprofen-loaded glyceryl monooleyl ether-based lyotropic liquid crystalline nanoparticles across the skin: Synchrotron X-ray diffraction and confocal laser scanning microscopy study
Study on the drug permeation mechanism from flurbiprofen-loaded glyceryl monooleyl ether-based lyotropic liquid crystalline nanoparticles across the skin: Synchrotron X-ray diffraction and confocal laser scanning microscopy study
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氟比洛芬甘油单油基醚溶致液晶纳米粒子皮肤药物渗透机制研究：同步加速器X射线衍射和共焦激光扫描显微镜研究
DOI：
10.1016/j.ijpharm.2018.11.031
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发表时间：
2019
影响因子：
5.8
通讯作者：
Kagawa Yoshiyuki
中科院分区：
文献类型：
--
作者：
Uchino Tomonobu;Kato Sayaka;Hatta Ichiro;Miyazaki Yasunori;Suzuki Tomonori;Sasaki Kohta;Kagawa Yoshiyuki
利用同步x射线衍射和共聚焦激光扫描显微镜（CLSM）研究了负载氟比洛芬（FLU）的六方结构甘油基单油基液晶纳米颗粒（LCNs）的皮肤渗透机制。用香豆素6和罗丹明B 1,2-二hexadecanoyl-sn-glycero-3-phosphoethanolamine， triethylamium salt （Rh-PE）制备荧光标记的flul负载lcn，它们分别产生绿色和红色荧光。在无毛小鼠角质层（SC）中应用负载了流感病毒的LCNs，导致六边形结构的晶格间距随着流感病毒的释放而扩大，这一点通过小角x射线衍射谱的变化得到了证实。此外，负载流感病毒的lcn在SC表面附近完全释放流感病毒，然后流感病毒穿透SC，因此，长周期相的重复距离略有改变。CLSM在表皮和毛囊中显示绿色荧光，SC中显示红色荧光。综上所述，llcn通过多种途径渗透，一种是部分通过细胞间基质，另一种是通过毛囊进入表皮。
The mechanism underlying the skin permeation of flurbiprofen (FLU)-loaded, glyceryl monooleyl ether-based liquid crystalline nanoparticles (LCNs) with a hexagonal structure was examined by synchrotron X-ray diffraction and confocal laser scanning microscopy (CLSM). Fluorescent-labeled, FLU-loaded LCNs were prepared using coumarin 6 and rhodamine B 1,2-dihexadecanoyl-sn-glycero-3-phosphoethanolamine, triethylammonium salt (Rh-PE), which produce green and red fluorescence, respectively. Application of FLU-loaded LCNs to the hairless mouse stratum corneum (SC) induced expansion of the lattice spacing of the hexagonal structure with FLU release, as confirmed by the changes in the small-angle X-ray diffraction profiles. In addition, the FLU-loaded LCNs completely released FLU near the surface of the SC, which then penetrated the SC. Consequently, the repeat distance of the long periodicity phase was slightly modified. CLSM revealed green fluorescence in the epidermis and hair follicles and red fluorescence in the SC. In conclusion, LCNs adopt several permeation pathways: one is partly via the intercellular matrix and the other is the epidermis via hair follicles.