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[1]王冉 史新元 杨树芳 戴幸星 乔延江.冰片对氟尿嘧啶经皮促透作用的多尺度研究[J].环球中医药,2017,10(05):517-522.[doi:10.3969/j.issn.1674-1749.2017.05.002]
　WANG ran,SHI Xinyuan,YANG Shufang,et al.Multi-scale study of borneol on the transdermal effect of fluorouracil[J].,2017,10(05):517-522.[doi:10.3969/j.issn.1674-1749.2017.05.002]
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冰片对氟尿嘧啶经皮促透作用的多尺度研究()
     
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《环球中医药》[ISSN:1006-6977/CN:61-1281/TN]

卷:
第10卷
期数:
2017年05期
页码:
517-522
栏目:
论著
出版日期:
2017-05-06

文章信息/Info

Title:
Multi-scale study of borneol on the transdermal effect of fluorouracil
作者:
王冉 史新元 杨树芳 戴幸星 乔延江
100069 北京,首都医科大学中医药学院[王冉(硕士研究生)]; 北京中医药大学中药信息工程研究中心(杨树芳、戴幸星、史新元、乔延江)
Author(s):
WANG ran;  SHI Xinyuan; YANG Shufang; et al.
School of Traditional Chinese Medicine, Capital Medical University, Beijing 100069, China
关键词:
冰片;  氟尿嘧啶;  促透作用;  分子动力学模拟;  多尺度方法
Keywords:
Borneol;  Fluorouracil;  Penetration enhancement;  Molecular dynamics simulations;  Multi-scale method
分类号:
R284
DOI:
10.3969/j.issn.1674-1749.2017.05.002
文献标志码:
A
摘要:
目的 研究冰片对氟尿嘧啶的经皮促透作用,探究冰片对亲水性药物的促透机理。方法 采用体外透皮实验、透射电子显微镜和介观分子动力学模拟等方法,分别对氟尿嘧啶的自身渗透性和冰片对其的促透作用进行多尺度研究。结果 氟尿嘧啶难以穿透角质层,最大渗透速率(0.82 μg/cm2)和单位面积累计渗透量(20.45 μg/cm2)均较低,在冰片的促透作用下,氟尿嘧啶的渗透速率和渗透量均增大,当冰片浓度为1%时,氟尿嘧啶的渗透速率[13.58 μg/(cm2·h)]和24小时单位面积累计渗透量(325.50 μg/cm2)较高,促渗比达16.57倍,且对角质层结构影响不大,为冰片促透氟尿嘧啶的最佳浓度; 冰片的促透作用主要表现为疏松角质层中脂质的排列,促进其中水通道的形成,从而促进氟尿嘧啶透过。结论 冰片可以促进亲水性氟尿嘧啶经皮渗透,其主要促透机理为疏松角质层脂质排列,促进水通道的形成。
Abstract:
Objective To investigate the penetration enhancement mechanism of borneolto on fluorouracil,and to explore the permeation mechanism of borneol on hydrophilic drugs.Methods The in vitro permeation experiments,transmission electron microscopic and microscopic molecular dynamics model was used to study the penetration of fluorouracil and the permeation enhancement of borneol.Results Fluorouracil was difficult to penetrate the stratum corneum,the maximum penetration rate was 0.82 μg/(cm2·h), and cumulative osmolality after 24h(20.45 μg/cm2)was low; with the enhancement effect of borneol, both penetration rate and cumulative osmolality of fluorouracil was increased, when the concentration of borneol was 1%, penetration rate[13.58 μg/(cm2·h)] and cumulative osmolality after 24h(325.50 μg/cm2)were the maximum value, the enhancement ratio was 16.57, and it had little effect on the stratum corneum structure, so 1% was the optimum concentration; Borneol can make the membrane lipid become loose and can promote the formation of water channels, thereby promoting the hydrophilic drugs penetration across. Conclusion Borneol can effectively promote the permeation of hydrophilic fluorouracil, the mechanism may be loosing the stratum corneum lipids and promoting the formation of water channels.

参考文献/References:

[1] 张宏梅,崔佰吉,钱曦垚,等.苯磺酸氨氯地平乳剂凝胶的制备及其体外透皮吸收的考察[J].中国新药杂志,2016,25(3):348-360.
[2] 许卫铭,王晖,李昕,等.蛇床子挥发油、薄荷醇及冰片对甲硝唑促透作用的比较[J].中南药学, 2006,4(2):111-113.
[3] 朱健平,王宗锐.龙脑促进药物经皮渗透作用的研究[J].中国药学杂志,1999,34(2):104-106.
[4] Huang L,Bai J,Yang H, et al. Combined use of borneolor menthol with labrasol promotespenetrationof baicalin through rabbit cornea in vitro[J].Pak J Pharm Sci,2015,28(1):1-7.
[5] Yi QF, Yan J, Tang SY, et al. Effect of borneol on the transdermal permeation of drugs with differing lipophilicity and molecular organization of stratum corneum lipids[J]. Drug Development and Industrial Pharmacy, 2016, 42(7):1086.
[6] 陈晓瑾,胡功允,梁文权. 四种药物的经皮渗透性能预测[J].中国现代应用药学杂志,2009,26(1):52-57.
[7] 解荣桂. 异维A酸联合0. 5%氟尿嘧啶软膏治疗顽固性扁平疣临床观察[J]. 中国美容医学,2013,22(6):685.
[8] 张海军. 氟尿嘧啶在皮肤科的几种新用途[J]. 医药导报,1994,15(3):115.
[9] Norlen L. Skin barrier structure and function: the single gel phase model[J]. J Invest Dermatol, 2001,117(4): 830-836.
[10] Das C, Olmsted PD, Noro MG. Water permeation through stratum corneum lipid bilayers from atomistic simulations[J]. Soft Matter, 2009, 5(22):4549-4555.
[11] 杨树芳,尹倩倩,史新元,等.基于计算机模拟的经皮给药研究中角质层脂质模型搭建及其稳定性考察[J].计算机与应用化学,2016,33(7):788-792.
[12] 邹浪,李晓芳,邓红,等.氟尿嘧啶的理化性质及透皮促渗剂对氟尿嘧啶经皮渗透的研究[J].江西中医学院学报,2013,25(6):63-66.
[13] 王景雁,兰颐,林红梅,等.薄荷醇对不同logP值中药有效成分经皮吸收的促透研究[J].中国新药杂志.2016,25(2):202-209.
[14] 赵茜,李伟泽,程玉钏,等.几种挥发油对黄藤素透皮给药的促渗作用研究[J].应用化工.2016,45(1):186-189.

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备注/Memo

备注/Memo:
基金项目: 国家自然科学基金(81473364); 北京市自然科学基金(7162122)
作者简介: 王冉(1992- ),女,2014级在读硕士研究生。研究方向:中药化学。E-mail:wangran2017@sina.com
通信作者: 乔延江(1956- ),博士,教授。研究方向:中药信息学。E-mail:yjqiao@263.net
更新日期/Last Update: 2017-05-06