Peng Qian, Xie Wen-Li, Chen Jing-Yi, Jiang Tao, Zhang Guo-Quan, Xu Zhong-Wei, Zhang Jin-Ning, Zhang Li
Logistics University of Chinese People's Armed Police Force, Department of Rescue Medicine, Teaching Section of Pharmacognosy and Pharmacy, Tianjin 300309, China.
Logistics University of Chinese People's Armed Police Force, Department of Clinical Medicine, Teaching Section of Pharmacology, Tianjin 300309, China.
Zhongguo Zhong Yao Za Zhi. 2018 May;43(9):1857-1863. doi: 10.19540/j.cnki.cjcmm.2018.0062.
To prepare the asiaticoside nanoemulsions (ASI-NEs) and asiaticoside nanoemulsions-based gels (ASI-NBGs), compare them with the commercial cream of asiaticoside (ASI-C) in terms of transdermal characteristics, and investigate the transdermal mechanism of ASI-NEs and ASI-NBGs. Their transdermal characteristics were studied by using Franz diffusion cells. The effect of topical ASI-NEs and ASI-NBGs on ultrastructure of rabbit skin was evaluated by using HE staining method. The localization and the permeation pathway of asiaticoside were visually investigated by using laser scanning confocal microscope (CLSM). The transdermal studies in vitro showed that the cumulative amount of ASI permeated from ASI-NEs and ASI-NBGs at 12 h after application were (3 504.30±180.93), (1 187.40±128.88) μg·cm⁻² respectively, 6.57, 2.23 times of that in the control group of ASI-C; the drug deposition of ASI-NEs and ASI-NBGs in skin was (159.48±7.47), (120.53±5.71) μg·cm⁻² respectively, 5.93, 4.48 times of that of ASI-C. HE staining of the rabbit skin after application of ASI-NEs and ASI-NBGs showed that the epidermis structure was basically intact; stratum corneum was loosed and the keratin fragment was increased; at the same time, the gap of prickle cell was increased and the basal cells were arranged loosely. The study of CLSM showed that significant percutaneous enhancer effect was observed for ASI-NEs after the topical application of 6 h, as the fluorescent compound was penetrated in the dermis and diffused uniformly. The fluorescence area and the integral optical density (IOD) were 28.81, 32.51 times of that in the FITC aqueous solution group, respectively. The fluorescent preparations showed strong fluorescence in the epidermis, but weak in deeper layers; with the increase of treatment time, the fluorescence in deeper layer was increased and stronger in skin appendages. The prepared ASI-NEs and ASI-NBGs have good transdermal characteristics and the transdermal mechanism is related to breaking the ultrastructure of stratum corneum and penetrating by the path of skin adnexa.
制备积雪草苷纳米乳剂（ASI-NEs）和积雪草苷纳米乳凝胶（ASI-NBGs），将它们与积雪草苷市售乳膏（ASI-C）在透皮特性方面进行比较，并研究ASI-NEs和ASI-NBGs的透皮机制。采用Franz扩散池研究它们的透皮特性。应用HE染色法评价局部应用ASI-NEs和ASI-NBGs对兔皮肤超微结构的影响。采用激光扫描共聚焦显微镜（CLSM）直观研究积雪草苷的定位及渗透途径。体外透皮研究表明，给药后12 h，ASI-NEs和ASI-NBGs中积雪草苷的累积渗透量分别为（3504.30±180.93）、（1187.40±128.88）μg·cm⁻²，分别是ASI-C对照组的6.57、2.23倍；ASI-NEs和ASI-NBGs在皮肤中的药物沉积量分别为（159.48±7.47）、（120.53±5.71）μg·cm⁻²，分别是ASI-C的5.93、4.48倍。应用ASI-NEs和ASI-NBGs后兔皮肤的HE染色显示，表皮结构基本完整；角质层疏松，角质碎片增多；同时，棘细胞间隙增大，基底细胞排列疏松。CLSM研究表明，局部应用6 h后，ASI-NEs观察到显著促渗作用，荧光化合物渗透至真皮并均匀扩散。荧光面积和积分光密度（IOD）分别是FITC水溶液组的28.81、32.51倍。荧光制剂在表皮显示强荧光，但在深层较弱；随着处理时间的增加，深层荧光增强，在皮肤附属器中更强。所制备的ASI-NEs和ASI-NBGs具有良好的透皮特性，其透皮机制与破坏角质层超微结构及通过皮肤附属器途径渗透有关。
