目的 考察天然及合成冰片对大黄素透皮吸收的影响。方法 首先用饱和溶液法,筛选适宜大黄素的供给液和接收液;采用Franz扩散池进行透皮实验,采用HPLC测定1~24 h时间内接收液中大黄素的量,以累积渗透量、渗透速率及增渗倍数为评价指标。结果 含有1%聚山梨酯80的80%乙醇生理盐水和60%乙醇生理盐水分别为供给液、接收液,可使大黄素溶解度提高到648 μg·mL-1并形成漏槽条件;大黄素渗透速率与其浓度呈正相关,为648 μg·mL-1＞569 μg·mL-1＞457 μg·mL-1;不同浓度天然及合成冰片对大黄素透皮吸收产生的影响分别为,2%＞3%＞1%＞空白对照组>4%、5%,2%＞4%＞1%＞空白对照组>3%、5%;2%天然冰片的稳态渗透速率为15.90 μg·cm-2·h-1,大于2%合成冰片的12.44 μg·cm-2·h-1。结论 天然及合成冰片的用量,决定了对大黄素透皮吸收的促渗或抑制作用,且天然冰片优于合成冰片。本结果为后续大黄素经皮促渗剂的选择提供了实验依据。
Abstract
OBJECTIVE To investigate the effect of natural and synthetic borneol on the transdermal absorption of emodin. METHODS The supplying and receiving solutions containing emodin were selected from the abdominal skin of mice in vitro, and the samples were analyzed by HPLC. The cumulative permeability, permeability rate and permeability enhancement factor were used as the evaluation indexes of the permeability enhancement effect. RESULTS The saline containing 1% Tween 80-80% ethanol and 60% ethanol could increase the solubility of emodin to 648 μg·mL-1 and obtain conditions of leaking trough. The penetration rate of emodin was 648 μg·mL-1＞569 μg·mL-1＞457 μg·mL-1 in the range of concentration. The penetration enhancement effect of synthetic borneol was 2%>4%>1%>blank control group>3% and 5%, and the steady-state permeation rates of 2% natural borneol (15.90 μg·cm-2·h-1) were higher than those of 2% synthetic borneol(12.44 μg·cm-2·h-1). CONCLUSION Natural borneol and synthetic borneol can promote the transdermal penetration of emodin, which is limited by their concentration. This provides an experimental basis for the selection of emodin transdermal enhancers.
关键词
大黄素 /
天然冰片 /
合成冰片 /
透皮吸收
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Key words
emodin /
natural borneol /
synthetic borneol /
transdermal absorption
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中图分类号：
R283
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参考文献
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脚注
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基金
国家自然科学海外及港澳学者合作研究基金资助(81728021);广东省自然科学基金资助(2016A030313573);2018年度大学生创新创业训练计划项目资助(57)
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