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包裹桑色素的脂质体:在PM诱导的角质形成细胞中理化性质、皮肤吸收改善及抗衰老活性的研究

Liposomes Encapsulating Morin: Investigation of Physicochemical Properties, Dermal Absorption Improvement and Anti-Aging Activity in PM-Induced Keratinocytes.

作者信息

Tran Hong-My, Yang Chun-Yin, Wu Tzu-Hui, Yen Feng-Lin

机构信息

Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.

School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.

出版信息

Antioxidants (Basel). 2022 Jun 16;11(6):1183. doi: 10.3390/antiox11061183.

DOI:10.3390/antiox11061183
PMID:35740084
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9229511/
Abstract

Recently, a global market for anti-aging skin care using botanicals has been noticeably developing. Morin, 3,5,7,2',4'-pentahydroxyflavone, is a polyphenol with many pharmacological properties including antioxidant, anti-inflammation and photoprotection. However, poor aqueous solubility of morin restricts its application in pharmaceuticals. The present study aimed to encapsulate morin into liposomal vesicles to improve its water solubility and skin penetration, and further investigated its ROS inhibition and anti-aging activity in HaCaT keratinocytes induced by particulate matters (PMs). Our data presented that morin was a strong DPPH radical scavenger. Morin displayed a remarkable ROS inhibitory ability and protected keratinocytes against PMs by downregulating matrix metalloproteinase-1 (MMP-1) expression via suppressing p-ERK and p-p38 in the MAPK pathway. Moreover, water solubility of liposomal morin (LM) prepared by the thin film hydration method was significantly better than free form of morin due to particle size reduction of LM. Our results also demonstrated that deformable liposomal vesicles were achieved for increasing dermal absorption. Additionally, LM (morin:lecinolws-50:tween-80:PF-68, 1:2.5:2.5:5) was able to effectively reduce generation of ROS, inactivate p-ERK, p-p38 and MMP-1 in HaCaT cells exposed to PM. In conclusion, our findings suggested that LM would be a bright candidate for various topical anti-aging and anti-pollution products.

摘要

最近,一个使用植物成分的抗老化护肤品全球市场正在显著发展。桑色素,即3,5,7,2',4'-五羟基黄酮,是一种具有多种药理特性的多酚,包括抗氧化、抗炎和光保护作用。然而,桑色素较差的水溶性限制了其在药物中的应用。本研究旨在将桑色素包封到脂质体囊泡中以提高其水溶性和皮肤渗透性,并进一步研究其在颗粒物(PMs)诱导的HaCaT角质形成细胞中的活性氧(ROS)抑制和抗老化活性。我们的数据表明桑色素是一种强大的二苯基苦味酰基自由基(DPPH)清除剂。桑色素表现出显著的ROS抑制能力,并通过抑制丝裂原活化蛋白激酶(MAPK)途径中的磷酸化细胞外信号调节激酶(p-ERK)和磷酸化p38,下调基质金属蛋白酶-1(MMP-1)的表达,从而保护角质形成细胞免受PMs的损伤。此外,通过薄膜水化法制备的脂质体桑色素(LM)由于粒径减小,其水溶性明显优于游离形式的桑色素。我们的结果还表明,可变形脂质体囊泡实现了增加皮肤吸收。此外,LM(桑色素:卵磷脂ws-50:吐温-80:泊洛沙姆-68,1:2.5:2.5:5)能够有效减少暴露于PM的HaCaT细胞中ROS的产生,使p-ERK、p-p38和MMP-1失活。总之,我们的研究结果表明,LM将是各种局部抗老化和抗污染产品的一个有前景的候选者。

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