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纳米脂质体载体作为用于生物活性成分的有前景的皮肤给药平台。

Nano-Liposomal Carrier as Promising Dermal Delivery Platform for L. Bioactives.

作者信息

Ahmoda Rabiea Ashowen, Milošević Milena, Marinković Aleksandar, Jovanović Aleksandra A

机构信息

Faculty of Technology and Metallurgy, University of Belgrade, 11000 Belgrade, Serbia.

Institute of Chemistry, Technology and Metallurgy-National Institute of the Republic of Serbia, University of Belgrade, 11000 Belgrade, Serbia.

出版信息

Pharmaceutics. 2025 Jun 14;17(6):782. doi: 10.3390/pharmaceutics17060782.

DOI:10.3390/pharmaceutics17060782
PMID:40574093
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12196744/
Abstract

This study investigates the physical, rheological, and antioxidant properties of nano-liposomal formulations encapsulating L. (fumitory) extract, focusing on their stability and performance under ultraviolet (UV) exposure, as well as polyphenol release within simulated skin conditions in a Franz diffusion cell. Liposomal formulations, composed of phospholipids with or without β-sitosterol or ergosterol, were evaluated for their encapsulation efficiency, liposome size, size distribution, zeta potential, viscosity, surface tension, density, oxidative stability, antioxidant capacity, and polyphenol recovery. Encapsulation efficiency was the highest in phospholipid liposomes (72.2%) and decreased with the incorporation of sterols: 66.7% for β-sitosterol and 62.9% for ergosterol liposomes. Encapsulation significantly increased viscosity and reduced surface tension compared to the plain liposomes, suggesting modified interfacial behavior. The inclusion of fumitory extract significantly increased the viscosity of liposomes (from ~2.5 to 6.09-6.78 mPa × s), consistent with the observed reduction in particle size and zeta potential. Antioxidant assays (thiobarbituric acid reactive substances-TBARS, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid-ABTS, and 2,2-diphenyl-1-picrylhydrazyl-DPPH) confirmed enhanced lipid peroxidation inhibition and radical scavenging upon encapsulation, with ABTS activity reaching up to 95.05% in sterol-containing liposomes. Release studies showed that the free extract exhibited the fastest polyphenol diffusion (5.09 × 10 m/s), while liposomes demonstrated slower/controlled release due to bilayer barriers. UV-irradiated liposomes released more polyphenols than untreated ones, particularly in the sterol-containing formulations, due to oxidative destabilization and pore formation. These findings highlight the potential of fumitory extract-loaded liposomes as stable, bioactive carriers with tunable polyphenol antioxidant release properties for dermal applications. Overall, liposomal formulations of fumitory extract exhibit significant potential for further development as a pharmaceutical, cosmetic, or dermo-cosmetic ingredient for use in the prevention and treatment of various skin disorders.

摘要

本研究考察了包封紫堇提取物的纳米脂质体制剂的物理、流变学和抗氧化性能,重点关注其在紫外线(UV)照射下的稳定性和性能,以及在Franz扩散池中模拟皮肤条件下的多酚释放情况。对由含或不含β-谷甾醇或麦角甾醇的磷脂组成的脂质体制剂进行了包封效率、脂质体大小、大小分布、zeta电位、粘度、表面张力、密度、氧化稳定性、抗氧化能力和多酚回收率的评估。磷脂脂质体的包封效率最高(72.2%),随着甾醇的加入而降低:β-谷甾醇脂质体为66.7%,麦角甾醇脂质体为62.9%。与普通脂质体相比,包封显著增加了粘度并降低了表面张力,表明界面行为发生了改变。加入紫堇提取物显著增加了脂质体的粘度(从~2.5增加到6.09 - 6.78 mPa·s),这与观察到的粒径和zeta电位的降低一致。抗氧化试验(硫代巴比妥酸反应物质 - TBARS、2,2'-联氮 - 双(3 - 乙基苯并噻唑啉 - 6 - 磺酸) - ABTS和2,2 - 二苯基 - 1 - 苦基肼 - DPPH)证实,包封后脂质过氧化抑制和自由基清除能力增强,含甾醇脂质体中的ABTS活性高达95.05%。释放研究表明,游离提取物表现出最快的多酚扩散速度(5.09×10 m/s),而脂质体由于双层屏障表现出较慢/可控的释放。紫外线照射的脂质体比未处理的脂质体释放更多的多酚,特别是在含甾醇的制剂中,这是由于氧化不稳定和孔隙形成。这些发现突出了负载紫堇提取物的脂质体作为稳定的生物活性载体的潜力,其具有可调节的多酚抗氧化释放特性,可用于皮肤应用。总体而言,紫堇提取物的脂质体制剂作为用于预防和治疗各种皮肤疾病的药物、化妆品或皮肤化妆品成分具有进一步开发的巨大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9549/12196744/9bd431e7bab9/pharmaceutics-17-00782-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9549/12196744/c0dfac515bc6/pharmaceutics-17-00782-g001a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9549/12196744/b10b695a90a2/pharmaceutics-17-00782-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9549/12196744/9bd431e7bab9/pharmaceutics-17-00782-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9549/12196744/c0dfac515bc6/pharmaceutics-17-00782-g001a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9549/12196744/b10b695a90a2/pharmaceutics-17-00782-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9549/12196744/9bd431e7bab9/pharmaceutics-17-00782-g003.jpg

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