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经纳米结构脂质载体调控的体内 β-胡萝卜素经皮渗透。

In vivo β-carotene skin permeation modulated by Nanostructured Lipid Carriers.

机构信息

Department of Life Sciences, University of Modena and Reggio Emilia, via G. Campi 103, 41125 Modena, Italy.

Department of Engineering "Enzo Ferrari", University of Modena and Reggio Emilia, via P. Vivarelli 10, 41125 Modena, Italy.

出版信息

Int J Pharm. 2021 Mar 15;597:120322. doi: 10.1016/j.ijpharm.2021.120322. Epub 2021 Feb 4.

DOI:10.1016/j.ijpharm.2021.120322
PMID:33549810
Abstract

Nanostructured Lipid Carriers (NLC) were investigated with the purpose of promoting skin permeation of the highly lipophilic β-carotene (BC) across the stratum corneum (SC) barrier so that it may perform its antioxidant properties in photo-aging and epithelial skin cancer prevention. Two differently sized NLC samples were developed using stearic acid and squalene as lipid matrix and evaluated in comparison with Microstructured Lipid Carriers (MLC). The carriers were characterized for morphology, size, Z-potential, BC loading and release as well as physical state by means of DSC and XRPD analyses. In vivo penetration of the carriers was assessed on humans by determining BC concentrations within the SC stratum disjunctum and stratum compactum layers removed by means of the tape stripping test in comparison with pure BC. Unlike MLC and pure BC that were mostly retained within the outermost layers of the SC, the NLC sample having the smallest size (about 200 nm) has proved to penetrate more deeply into the SC barrier. Accordingly, the goal of providing β-carotene actions against oxidative damages within the looser skin viable tissues could be envisaged.

摘要

纳米结构脂质载体 (NLC) 被研究用于促进高度亲脂性β-胡萝卜素 (BC) 通过角质层 (SC) 屏障的皮肤渗透,以便其在光老化和上皮皮肤癌预防中发挥抗氧化特性。使用硬脂酸和角鲨烯作为脂质基质开发了两种不同大小的 NLC 样品,并与微结构化脂质载体 (MLC) 进行了比较。通过 DSC 和 XRPD 分析对载体的形态、大小、Z 电位、BC 负载和释放以及物理状态进行了表征。通过胶带剥离试验从 SC 角质层分离层和致密层中去除,在人体上评估了载体的体内渗透,以确定 SC 层中的 BC 浓度,并与纯 BC 进行了比较。与主要保留在 SC 最外层的 MLC 和纯 BC 不同,粒径最小(约 200nm)的 NLC 样品已被证明能更深入地渗透到 SC 屏障中。因此,可以设想提供β-胡萝卜素以对抗疏松皮肤活组织中的氧化损伤。

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