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水包油型乳剂会损害角质层屏障并提高药物渗透性。

O/W emulsions compromise the stratum corneum barrier and improve drug penetration.

作者信息

Gloor M, Hauth A, Gehring W

机构信息

Department of Dermatology, Klinikum der Stadt Karlsruhe GmbH, Germany.

出版信息

Pharmazie. 2003 Oct;58(10):709-15.

Abstract

BACKGROUND

W/O emulsions improve the stratum corneum barrier, while microemulsions tend to compromise it. We, therefore, were interested to explore the effects of O/W emulsions on the stratum corneum barrier.

METHODS

Aqueous Cream BP 2001, Clioquinol Cream BP 1999 without clioquinol, Nonionic Hydrophilic Cream DAB 2001 without glycerol, Hydrophilic Skin Emulsion Base NRF S. 25., point of time 2001, without glycerol, and Base Cream DAC were tested versus untreated controls in 29 healthy volunteers for 7 days. Outcome measures included transepidermal water loss (TEWL), skin redness (chromametry a*-value) and erythrocyte circulation in the subpapillary vessels (laser Doppler). Barrier compromise was subsequently explored by performing the hydrocortisone blanching test using Hydrocortisone Cream 0.5% NRF 11.36. (outcome measure: a*-value) in 15 subjects and the sodium lauryl sulfate (SLS) irritation test (outcome measures: TEWL, a*-value, laser Doppler) in 14 subjects.

RESULTS

Pretreatment with the test emulsions produced increases in TEWL (statistically significant for all test emulsions), a*-value (statistically significant for Aqueous Cream BP 2001 and Base Cream DAC), and laser Doppler value (statistically significant for all emulsions except Base Cream DAC). Hydrocortisone penetration was statistically significantly increased with all test emulsions versus untreated contols. SLS irritation was mostly statistically significantly increased versus untreated controls when analyzing the study endpoint-baseline difference.

CONCLUSIONS

O/W emulsions may compromise the stratum corneum barrier and improve drug penetration.

摘要

背景

油包水型乳液可改善角质层屏障功能,而微乳液往往会损害该功能。因此,我们有兴趣探究水包油型乳液对角质层屏障的影响。

方法

选取29名健康志愿者,将2001版英国药典水性乳膏、不含氯碘羟喹的1999版英国药典氯碘羟喹乳膏、不含甘油的2001版德国药典非离子亲水性乳膏、不含甘油的2001版日本药局方亲水性皮肤乳液基质以及德国药典基础乳膏与未处理的对照品进行7天的对比测试。观察指标包括经皮水分流失(TEWL)、皮肤发红(色度计a值)以及乳头下血管中的红细胞循环(激光多普勒)。随后,在15名受试者中使用0.5%的11.36版日本药局方氢化可的松乳膏进行氢化可的松变白试验(观察指标:a值),并在14名受试者中进行月桂醇硫酸酯钠(SLS)刺激试验(观察指标:TEWL、a*值、激光多普勒),以探究屏障受损情况。

结果

用受试乳液预处理后,TEWL升高(所有受试乳液均具有统计学意义),a*值升高(2001版英国药典水性乳膏和德国药典基础乳膏具有统计学意义),激光多普勒值升高(除德国药典基础乳膏外的所有乳液均具有统计学意义)。与未处理的对照品相比,所有受试乳液的氢化可的松渗透率均有统计学意义的显著提高。在分析研究终点与基线的差异时,与未处理的对照品相比,SLS刺激大多具有统计学意义的显著增加。

结论

水包油型乳液可能会损害角质层屏障并提高药物渗透性。

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