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经皮水分散失的体外和体内评估:药物经皮给药系统应用于药物分析。

In vitro and in vivo trans-epidermal water loss evaluation following topical drug delivery systems application for pharmaceutical analysis.

机构信息

Department of Experimental and Clinical Medicine, University of Catanzaro "Magna Graecia", Viale Europa s.n.c., I-88100, Catanzaro, Italy.

Department of Health Sciences, University of Catanzaro "Magna Graecia", Viale Europa s.n.c., I-88100, Catanzaro, Italy.

出版信息

J Pharm Biomed Anal. 2020 Jul 15;186:113295. doi: 10.1016/j.jpba.2020.113295. Epub 2020 Apr 17.

Abstract

The measurement of Trans-Epidermal Water Loss (TEWL) allows to evaluate the integrity of Stratum Corneum Epidermis (SCE) barrier after topical application of colloidal nanocarriers by using a non-invasive method. The temporarily modifications of SCE lipids are important for the passage of colloidal nanocarriers across the skin; this passage causes a modification of TEWL values. Niosomes, ethosomes®, and transfersomes® are used as topical drug delivery systems due to their biopharmaceutical properties, and capability to permeate intact through the SCE. In vitro and in vivo evaluation of TEWL values was studied for niosomes, ethosomes® and transfersomes® in occlusive and non-occlusive conditions. TEWL values in vivo, using healthy human volunteers, are ∼12 g/m∙× h for all nanoformulations after 72 h, due to the rearrangement of lipids forming the SCE membranes. Conversely, TEWL values of healthy human volunteers, that are topically treated with niosomes, ethosomes® and transfersomes®, in non-occlusive conditions, are ∼20 g/m∙× h. This data was lower than those obtained in occlusive conditions (∼35 g/m∙× h). In vitro studies agreed results which are obtained in occlusive conditions using healthy human volunteers. SCE lipids of the skin restore their native structure after 72 h of nanocarrier application. In vitro and in vivo results showed that niosomes, ethosomes®, and transfersomes® interact with the skin in a temporary and reversible mode, and they can be used as suitable colloidal nanocarriers to increase the percutaneous permeation of drugs after topical application without damaging the native structure of the skin.

摘要

经皮水分流失(TEWL)的测量可用于评估胶体纳米载体经皮给药后角质层表皮(SCE)屏障的完整性,采用非侵入性方法。SCE 脂质的暂时改变对于胶体纳米载体穿过皮肤很重要;这种通过会导致 TEWL 值的改变。由于具有生物制药特性以及能够完整地穿透 SCE,因此将非离子型脂质体、醇质体和传递体用作局部药物递送系统。在密闭和非密闭条件下,对非离子型脂质体、醇质体和传递体的 TEWL 值进行了体外和体内评估。在非密闭条件下,使用健康的人类志愿者,所有纳米制剂在 72 小时后体内的 TEWL 值约为 12g/m∙× h,这是由于形成 SCE 膜的脂质重新排列所致。相反,在非密闭条件下,用非离子型脂质体、醇质体和传递体局部处理的健康人类志愿者的 TEWL 值约为 20g/m∙× h。该数据低于在密闭条件下(约 35g/m∙× h)获得的数据。在密闭条件下使用健康的人类志愿者进行的体外研究结果与体内研究结果一致。皮肤的 SCE 脂质在纳米载体应用 72 小时后恢复其天然结构。体外和体内结果表明,非离子型脂质体、醇质体和传递体与皮肤以暂时和可逆的方式相互作用,并且它们可以用作合适的胶体纳米载体,以增加经皮给药后药物的经皮渗透,而不会破坏皮肤的天然结构。

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