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用于将活性分子递送至皮肤内并透过皮肤的成膜系统。

Film Forming Systems for Delivery of Active Molecules into and across the Skin.

作者信息

Touitou Elka, Natsheh Hiba, Zailer Jana

机构信息

The Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Ein Karem, Jerusalem 9112102, Israel.

出版信息

Pharmaceutics. 2023 Jan 24;15(2):397. doi: 10.3390/pharmaceutics15020397.

DOI:10.3390/pharmaceutics15020397
PMID:36839719
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9967029/
Abstract

We have investigated delivery systems that can form a structured matrix film on the skin after their application. In a previous work, we have shown that Weblike film forming systems (also called Pouches Drug Delivery Systems, PDDS) enable enhanced skin delivery of the incorporated molecules. These delivery systems are composed of one or more phospholipids, a short-chain alcohol, a polymer and optionally water. In this work, we continue the investigation and characterization of Weblike carriers focusing on some factors affecting the delivery properties such as components concentration and mode of application on the skin. Upon non-occluded application on the skin, the systems dry rapidly, forming a web-like structured film. Lidocaine, Ibuprofen, FITC and Cannabidiol are molecules with various physico-chemical properties that were incorporated in the carrier. The systems were tested in a number of in vitro and in vivo experiments. Results of the in vitro permeation of Ibuprofen through porcine skin indicated two-fold delivery through the skin of Ibuprofen when applied from our Weblike system in comparison with a nanovesicular carrier, the ethosome. We also have investigated weblike systems containing hemp seed oil (HSO). This addition enhanced the film's ability to deliver lipophilic molecules to the deeper skin layers, leading to an improved pharmacodynamic effect. In analgesic tests carried out in a pain mice model following one hour application of CBD in Weblike system with and without HSO, the number of writhing episodes was decreased from 29 in the untreated animals to 9.5 and 18.5 writhes, respectively. The results of our work open the way towards a further investigation of Weblike film forming systems containing drugs for improved dermal and transdermal treatment of various ailments.

摘要

我们研究了在应用后能在皮肤上形成结构化基质膜的递送系统。在之前的工作中,我们已经表明,网状成膜系统(也称为袋式药物递送系统,PDDS)能够增强所包裹分子的皮肤递送。这些递送系统由一种或多种磷脂、短链醇、聚合物以及视情况而定的水组成。在这项工作中,我们继续对网状载体进行研究和表征,重点关注一些影响递送特性的因素,如成分浓度和在皮肤上的应用方式。在皮肤非封闭应用时,这些系统迅速干燥,形成网状结构化膜。利多卡因、布洛芬、异硫氰酸荧光素(FITC)和大麻二酚是具有各种物理化学性质的分子,它们被包裹在载体中。这些系统在一系列体外和体内实验中进行了测试。布洛芬通过猪皮肤的体外渗透结果表明,与纳米泡囊载体(醇质体)相比,从我们的网状系统应用时,布洛芬通过皮肤的递送量增加了两倍。我们还研究了含有大麻籽油(HSO)的网状系统。这种添加增强了膜将亲脂性分子递送到皮肤深层的能力,从而产生了改善的药效学效果。在疼痛小鼠模型中进行的镇痛测试中,在应用含或不含HSO的网状系统中的CBD一小时后,扭体发作次数从未经治疗动物的29次分别减少到9.5次和18.5次。我们的工作结果为进一步研究含有药物的网状成膜系统以改善各种疾病的皮肤和透皮治疗开辟了道路。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/cf1a0265fba2/pharmaceutics-15-00397-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/94f682c68c2c/pharmaceutics-15-00397-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/7369eb8c7c29/pharmaceutics-15-00397-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/a4e6ddf6b3d9/pharmaceutics-15-00397-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/e008fa8edddb/pharmaceutics-15-00397-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/ed4b9b1dfd0b/pharmaceutics-15-00397-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/4d694839f34e/pharmaceutics-15-00397-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/cf1a0265fba2/pharmaceutics-15-00397-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/94f682c68c2c/pharmaceutics-15-00397-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/7369eb8c7c29/pharmaceutics-15-00397-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/a4e6ddf6b3d9/pharmaceutics-15-00397-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/e008fa8edddb/pharmaceutics-15-00397-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/ed4b9b1dfd0b/pharmaceutics-15-00397-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/4d694839f34e/pharmaceutics-15-00397-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b138/9967029/cf1a0265fba2/pharmaceutics-15-00397-g007.jpg

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