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化妆品中视黄醇半固体制剂:经皮渗透机制和行为。

Retinol semisolid preparations in cosmetics: transcutaneous permeation mechanism and behaviour.

机构信息

HBN Research Institute and Biological Laboratory, Shenzhen Hujia Technology Co., Ltd, Shenzhen, 518000, Guangdong, People's Republic of China.

State Key Laboratory of Bioactive Molecules and Druggability Assessment, Jinan University, Guangzhou, 510632, China.

出版信息

Sci Rep. 2024 Oct 1;14(1):22793. doi: 10.1038/s41598-024-73240-y.

Abstract

Retinol is widely used to treat skin ageing because of its effect on cell differentiation, proliferation and apoptosis. However, its potential benefits appear to be limited by its skin permeability. Herein, we investigated the transcutaneous behavior of retinol in semisolid cosmetics, in both in vitro and in vivo experiments. In vitro experiments used the modified Franz diffusion cell combined with Raman spectroscopy. In in vivo experiments, the content of retinol in rat skin and plasma was detected with HPLC. Retinol in semisolid cosmetics was mainly concentrated in the stratum corneum in the skin of the three animal models tested, and in any case did not cross the skin barrier after a 24 h dermatologic topical treatment in Franz diffusion cells tests. Similar results were obtained in live mice and rats, where retinol did not cross the skin barrier and did not enter the blood circulation. Raman spectroscopy was used to test the penetration depth of retinol in skin, which reached 16 μm out of 34 μm in pig skin, whereas the skin of mouse and rat showed too strong bakground interference. To explore epidermal transport mechanism and intradermal residence, skin transcriptomics was performed in rats, which identified 126 genes upregulated related to retinol transport and metabolism, relevant to the search terms "retinoid metabolic process" and "transporter activity". The identity of these upregulated genes suggests that the mechanism of retinol action is linked to epidermis, skin, tissue and epithelium development.

摘要

视黄醇因其对细胞分化、增殖和凋亡的影响而被广泛用于治疗皮肤衰老。然而,其潜在的益处似乎受到皮肤通透性的限制。在此,我们研究了视黄醇在半固体化妆品中的经皮行为,包括在体外和体内实验中。体外实验采用改良的Franz 扩散池结合拉曼光谱法。在体内实验中,采用 HPLC 检测大鼠皮肤和血浆中的视黄醇含量。半固体化妆品中的视黄醇主要集中在三种动物模型皮肤的角质层中,并且在Franz 扩散池测试中,经皮局部治疗 24 小时后,无论如何都不会穿过皮肤屏障。在活体小鼠和大鼠中也得到了类似的结果,视黄醇没有穿过皮肤屏障,也没有进入血液循环。拉曼光谱用于测试视黄醇在皮肤中的渗透深度,在猪皮中达到 34 μm 的 16 μm,而小鼠和大鼠的皮肤则表现出太强的背景干扰。为了探索表皮转运机制和真皮内滞留,对大鼠进行皮肤转录组学研究,鉴定出 126 个与视黄醇转运和代谢相关的上调基因,与“类视黄醇代谢过程”和“转运蛋白活性”等检索词相关。这些上调基因的存在表明视黄醇的作用机制与表皮、皮肤、组织和上皮发育有关。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2adb/11445495/cd6ee31d0ee7/41598_2024_73240_Fig1_HTML.jpg

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