摘要
制备积雪草苷纳米乳（asiaticoside nanoemulsions,ASI-NEs）及纳米乳凝胶（asiaticoside nanoemulsions-based gels,ASINBGs）,与市售软膏进行体外透皮特性比较,并研究ASI-NEs和ASI-NBGs的透皮机制。采用Franz扩散池研究ASI-NEs和ASI-NBGs的体外透皮特性,HE染色法考察家兔局部给药对皮肤微观结构的影响,激光扫描共聚焦显微镜（CLSM）可视化研究药物的分布及渗透行为。体外透皮结果表明,经皮给药12 h,ASI-NEs和ASI-NBGs单位面积累积渗透量分别是（3 504.30±180.93）,（1 187.40±128.88）μg·cm-2,是市售软膏对照组的6.57,2.23倍,皮肤滞留量分别是（159.48±7.47）,（120.53±5.71）μg·cm-2,是市售软膏对照组的5.93,4.48倍;HE染色发现,使用ASI-NEs和ASI-NBGs后,表皮结构基本完整,角质疏松变薄,角蛋白碎片增多,棘层细胞间隙增大,基底层细胞排列松散。CLSM研究显示,FITC荧光探针标记的ASINEs皮肤渗透快,用药6 h即在真皮均匀分布,荧光面积和积分光密度（IOD）分别是FITC水溶液对照组的28.81,32.51倍。各荧光制剂在皮肤表皮荧光较强,深处较弱,随治疗时间延长,深层荧光增加,且在皮肤附属器部位荧光较强。制备的ASINEs和ASI-NBGs具有良好透皮特性,其透皮机制主要是通过破坏皮肤角质层微观结构和借助皮肤附属器途径,使药物透过皮肤发挥治疗作用。
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.
作者
彭倩
谢文利
陈静怡
江涛
张国权
徐忠伟
张津宁
张莉
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;Logistics University of Chinese People＇s Armed Police Force, Department of Clinical Medicine, Teaching Section of Anatoray, Tianjin 300309, China;Logistics University of Chinese People＇s Armed Police Force, Central Laboratory of R＆D Department, Tianjin 300309, China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2018年第9期1857-1863,共7页
China Journal of Chinese Materia Medica
基金
武警后勤学院基础研究项目(WHJ2015012,WHJ201501)
作者简介
彭倩，硕士研究生，研究方向为微粒给药系统，E-mail：2285289469@qq．com;谢文利，教授，研究方向为药理学，E-mail：xiewenli5@sohu．com;[通信作者]张莉，教授，研究方向为药物新剂型，E-mail：zhli62tianjin@163．com.
