Efficacy and safety of permeation enhancers: A kinetic evaluation approach and molecular mechanism study in the skin

渗透 角质层 亲脂性 化学 刺激 红斑 色谱法 体内 生物物理学 立体化学 生物化学 皮肤病科 医学 免疫学 生物技术 病理 生物
作者
Jiuheng Ruan,Chao Liu,Jiaqi Wang,Ting Zhong,Peng Quan,Liang Fang
出处
期刊:International Journal of Pharmaceutics [Elsevier BV]
卷期号:626: 122155-122155 被引量:22
标识
DOI:10.1016/j.ijpharm.2022.122155
摘要

This study sought to provide approach for evaluating and predicting the efficacy and safety of permeation enhancers on the basis of their kinetic distribution behavior in the skin dictated by physicochemical properties. Herein, the efficacy-safety regularity of eight permeation enhancers were studied with ex vivo skin permeation study, small-angle X-ray scattering, MTT assay, H&E staining, and in vivo skin erythema analysis, classifying into the following three categories: high enhancement-low irritation, medium enhancement-high irritation, and low enhancement-low irritation. These three modes were positively correlated with the distribution amount of permeation enhancers in the skin layers and verified by the in vitro tape-stripping study. The kinetic parameter, effective-safety index (IES), was proposed to describe the regularity of enhancement effect tendency and irritation risk, and the relationship between IES and physicochemical properties of permeation enhancers was analyzed with multiple regression analysis. According to the results of modulated temperature differential scanning calorimetry and dielectric spectrum, permeation enhancers with high lipophilicity and low polarity had IES > 1, suggesting high enhancement effect and low irritation due to their higher affinity with the stratum corneum (SC) than with epidermis (EP). Permeation enhancers with medium lipophilicity and medium polarity exhibited 0 < IES ≤ 1, showing medium enhancement effect and high irritation, as determined by their comparable affinity with the SC and epidermis (EP). However, permeation enhancers with low lipophilicity and high polarity had IES → 0, demonstrating low enhancement effect and irritation, as indicated by their poor affinity with the SC. In summary, different physicochemical properties of permeation enhancers influenced their affinities with skin layers, resulting in their different enhancement effect and irritation potential. This study will provide a theoretical basis and criteria for evaluating and predicting the safety and efficacy of permeation enhancers, which will enable a more rational selection of permeation enhancers in the optimization of transdermal patches.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
PDF的下载单位、IP信息已删除 (2025-6-4)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
1秒前
青争完成签到,获得积分10
1秒前
2秒前
2秒前
Jhinnnn完成签到,获得积分10
3秒前
3秒前
3秒前
123完成签到,获得积分10
3秒前
木木林完成签到 ,获得积分10
5秒前
笨笨摇伽发布了新的文献求助10
6秒前
wangyue发布了新的文献求助10
6秒前
lm完成签到 ,获得积分10
7秒前
个性的海之完成签到,获得积分20
7秒前
科研通AI2S应助zouni采纳,获得10
7秒前
8秒前
Ternura发布了新的文献求助10
8秒前
llll发布了新的文献求助10
8秒前
9秒前
王军鹏发布了新的文献求助20
9秒前
可爱的函函应助凉茶采纳,获得10
11秒前
12秒前
12秒前
witty完成签到,获得积分0
13秒前
qwq完成签到,获得积分10
13秒前
爆米花应助方格采纳,获得10
13秒前
淡淡菠萝完成签到 ,获得积分10
14秒前
量子星尘发布了新的文献求助10
14秒前
陈昊发布了新的文献求助10
15秒前
耿春丽发布了新的文献求助10
15秒前
麦克尔完成签到,获得积分10
15秒前
c程序语言完成签到,获得积分10
16秒前
17秒前
17秒前
18秒前
18秒前
Mr.Jian完成签到,获得积分10
19秒前
呼君伟完成签到,获得积分10
19秒前
Vera完成签到,获得积分10
20秒前
上官若男应助白术采纳,获得10
22秒前
lll发布了新的文献求助10
22秒前
高分求助中
A new approach to the extrapolation of accelerated life test data 1000
ACSM’s Guidelines for Exercise Testing and Prescription, 12th edition 500
‘Unruly’ Children: Historical Fieldnotes and Learning Morality in a Taiwan Village (New Departures in Anthropology) 400
Indomethacinのヒトにおける経皮吸収 400
Phylogenetic study of the order Polydesmida (Myriapoda: Diplopoda) 370
基于可调谐半导体激光吸收光谱技术泄漏气体检测系统的研究 350
Robot-supported joining of reinforcement textiles with one-sided sewing heads 320
热门求助领域 (近24小时)
化学 材料科学 医学 生物 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 遗传学 基因 物理化学 催化作用 冶金 细胞生物学 免疫学
热门帖子
关注 科研通微信公众号,转发送积分 3988827
求助须知:如何正确求助?哪些是违规求助? 3531197
关于积分的说明 11252739
捐赠科研通 3269830
什么是DOI,文献DOI怎么找? 1804815
邀请新用户注册赠送积分活动 881915
科研通“疑难数据库(出版商)”最低求助积分说明 809028