{"title":"使用从啤酒糟中提取的阿魏酸脂质囊泡在体内减轻皮肤炎症。","authors":"","doi":"10.1016/j.ijpharm.2024.124764","DOIUrl":null,"url":null,"abstract":"<div><div>Breweŕs spent grain (BSG) is the main by-product of the brewing industry, and due to its rapid decomposition, it generates serious environmental problems such as malodors and greenhouse gases emissions. On the other hand, this lignocellulosic compound contains a large number of antioxidants, being ferulic acid (FA) the most abundant. FA is a powerful antioxidant molecule that has demonstrated significant protective effects on key components of the skin, including keratinocytes, fibroblasts, collagen, and elastin. FA inhibits melanogenesis, promotes angiogenesis and accelerates the wound healing although its use is limited by its rapid oxidation. In this study, different hydrolysis treatments (chemical, enzymatic and hydrothermal) were performed on BSG to obtain FA. Herein FA-loaded ultradeformable liposomes (ULs) were designed to improve their stability and <em>in vivo</em> performance. These nanosystems allow FA permeability through human skin, as proven by an <em>ex vivo</em> skin permeability assay using Franz diffusion cells. The toxicity and anti-inflammatory activity of the formulation has been investigated. The free form and 100 nm FA_ULs were evaluated. Cell viability was dose-dependent and provided optimal results for the treatment of inflammatory skin conditions in an <em>in vivo</em> Oxazolone-induced Delayed Type Hypersensitivity model using Swiss CD1 mice, demonstrated by the reduction of the inflammatory cytokines expression, ear thickness, bioluminescence and histological evaluation. These results pave the way for FA-based treatments of skin and inflammatory conditions.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3000,"publicationDate":"2024-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"In vivo reduction of skin inflammation using ferulic acid-loaded lipid vesicles derived from Brewer’s spent grain\",\"authors\":\"\",\"doi\":\"10.1016/j.ijpharm.2024.124764\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Breweŕs spent grain (BSG) is the main by-product of the brewing industry, and due to its rapid decomposition, it generates serious environmental problems such as malodors and greenhouse gases emissions. On the other hand, this lignocellulosic compound contains a large number of antioxidants, being ferulic acid (FA) the most abundant. FA is a powerful antioxidant molecule that has demonstrated significant protective effects on key components of the skin, including keratinocytes, fibroblasts, collagen, and elastin. FA inhibits melanogenesis, promotes angiogenesis and accelerates the wound healing although its use is limited by its rapid oxidation. In this study, different hydrolysis treatments (chemical, enzymatic and hydrothermal) were performed on BSG to obtain FA. Herein FA-loaded ultradeformable liposomes (ULs) were designed to improve their stability and <em>in vivo</em> performance. These nanosystems allow FA permeability through human skin, as proven by an <em>ex vivo</em> skin permeability assay using Franz diffusion cells. The toxicity and anti-inflammatory activity of the formulation has been investigated. The free form and 100 nm FA_ULs were evaluated. Cell viability was dose-dependent and provided optimal results for the treatment of inflammatory skin conditions in an <em>in vivo</em> Oxazolone-induced Delayed Type Hypersensitivity model using Swiss CD1 mice, demonstrated by the reduction of the inflammatory cytokines expression, ear thickness, bioluminescence and histological evaluation. 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引用次数: 0
摘要
啤酒糟(BSG)是酿造业的主要副产品,由于其分解速度快,会产生严重的环境问题,如恶臭和温室气体排放。另一方面,这种木质纤维素化合物含有大量抗氧化剂,其中阿魏酸(FA)含量最高。阿魏酸是一种强大的抗氧化分子,对皮肤的主要成分,包括角质细胞、成纤维细胞、胶原蛋白和弹性蛋白具有显著的保护作用。FA 可抑制黑色素生成、促进血管生成并加速伤口愈合,但其快速氧化限制了它的使用。本研究对 BSG 进行了不同的水解处理(化学、酶解和水热),以获得 FA。在此基础上,设计了负载 FA 的超变形脂质体(ULs),以提高其稳定性和体内性能。利用弗朗兹扩散细胞进行的体内外皮肤渗透性试验证明,这些纳米系统可使 FA 通过人体皮肤渗透。对配方的毒性和抗炎活性进行了研究。对自由形态和 100 纳米 FA_UL 进行了评估。在使用瑞士 CD1 小鼠进行的体内 Oxazolone 诱导的延迟型超敏反应模型中,通过减少炎症细胞因子的表达、耳厚度、生物发光和组织学评估,证明细胞活力与剂量有关,并为炎症性皮肤状况的治疗提供了最佳结果。这些结果为基于 FA 的皮肤和炎症治疗铺平了道路。
In vivo reduction of skin inflammation using ferulic acid-loaded lipid vesicles derived from Brewer’s spent grain
Breweŕs spent grain (BSG) is the main by-product of the brewing industry, and due to its rapid decomposition, it generates serious environmental problems such as malodors and greenhouse gases emissions. On the other hand, this lignocellulosic compound contains a large number of antioxidants, being ferulic acid (FA) the most abundant. FA is a powerful antioxidant molecule that has demonstrated significant protective effects on key components of the skin, including keratinocytes, fibroblasts, collagen, and elastin. FA inhibits melanogenesis, promotes angiogenesis and accelerates the wound healing although its use is limited by its rapid oxidation. In this study, different hydrolysis treatments (chemical, enzymatic and hydrothermal) were performed on BSG to obtain FA. Herein FA-loaded ultradeformable liposomes (ULs) were designed to improve their stability and in vivo performance. These nanosystems allow FA permeability through human skin, as proven by an ex vivo skin permeability assay using Franz diffusion cells. The toxicity and anti-inflammatory activity of the formulation has been investigated. The free form and 100 nm FA_ULs were evaluated. Cell viability was dose-dependent and provided optimal results for the treatment of inflammatory skin conditions in an in vivo Oxazolone-induced Delayed Type Hypersensitivity model using Swiss CD1 mice, demonstrated by the reduction of the inflammatory cytokines expression, ear thickness, bioluminescence and histological evaluation. These results pave the way for FA-based treatments of skin and inflammatory conditions.
期刊介绍:
The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.