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用于局部应用中3-O-乙基-L-抗坏血酸递送的脂质基凝胶

Lipid-Based Gels for Delivery of 3-O-Ethyl L-Ascorbic acid in Topical Applications.

作者信息

Loza-Rodríguez Noèlia, Millán-Sánchez Aina, Mallandrich Mireia, Calpena Ana Cristina, López Olga

机构信息

Department of Chemical and Surfactant Technology, Institute of Advanced Chemistry of Catalonia (IQAC-CSIC), C/Jordi Girona 18-26, 08034 Barcelona, Spain.

Bicosome S.L., C/Jordi Girona 18-26, 08034 Barcelona, Spain.

出版信息

Pharmaceutics. 2024 Sep 7;16(9):1187. doi: 10.3390/pharmaceutics16091187.

DOI:10.3390/pharmaceutics16091187
PMID:39339223
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11435238/
Abstract

This study explores the incorporation of 10% 3-O-ethyl L-ascorbic acid (ETVC), a derivative of vitamin C, into two lipid gel systems: a hydrogel (HG) consisting exclusively of lipids and water and a bigel (BG) combining the hydrogel with an oleogel made from olive oil and beeswax. We investigated the ETVC release profiles from both materials using synthetic membranes and measured their permeation through porcine skin in vitro. Additionally, the interaction of these lipid gel systems with the stratum corneum (SC) was determined. Results from the release study indicate that the BG exhibited slower ETVC release compared to the HG. The permeation experiments showed that the presence of lipids in the formulations enhanced ETVC retention in the skin. The HG delivered a higher amount to the SC, while the BG achieved greater retention in the epidermis. This difference is attributed to the different lipophilic nature of each material. The structural analysis of SC lipids revealed that the organization of surface lipids remained unaltered by the application of the gels. Finally, an in vitro efficacy test in porcine skin using methylene blue indicated that our ETVC gels exhibited antioxidant activity. These findings provide valuable insights into the potential of lipid-based gels for topical applications.

摘要

本研究探讨了将维生素C的衍生物10% 3 - O - 乙基 - L - 抗坏血酸(ETVC)掺入两种脂质凝胶体系:一种是仅由脂质和水组成的水凝胶(HG),另一种是将水凝胶与由橄榄油和蜂蜡制成的油凝胶相结合的双凝胶(BG)。我们使用合成膜研究了两种材料中ETVC的释放曲线,并在体外测量了它们透过猪皮肤的渗透率。此外,还测定了这些脂质凝胶体系与角质层(SC)的相互作用。释放研究结果表明,与HG相比,BG的ETVC释放较慢。渗透实验表明,制剂中脂质的存在增强了ETVC在皮肤中的保留。HG向SC输送的量更高,而BG在表皮中的保留量更大。这种差异归因于每种材料不同的亲脂性。SC脂质的结构分析表明,凝胶的应用未改变表面脂质的组织。最后,在猪皮肤上使用亚甲蓝进行的体外功效测试表明,我们的ETVC凝胶具有抗氧化活性。这些发现为基于脂质的凝胶在局部应用中的潜力提供了有价值的见解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/dd41f9ad53c1/pharmaceutics-16-01187-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/89f84ec813a6/pharmaceutics-16-01187-g0A1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/6cef41f2b902/pharmaceutics-16-01187-g0A2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/445661466f23/pharmaceutics-16-01187-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/2fc6763faff0/pharmaceutics-16-01187-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/c60dc975196e/pharmaceutics-16-01187-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/9a6967dcb0bc/pharmaceutics-16-01187-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/589d1812e4d2/pharmaceutics-16-01187-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/be88c066cfda/pharmaceutics-16-01187-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/dd41f9ad53c1/pharmaceutics-16-01187-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/89f84ec813a6/pharmaceutics-16-01187-g0A1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/6cef41f2b902/pharmaceutics-16-01187-g0A2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/445661466f23/pharmaceutics-16-01187-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/2fc6763faff0/pharmaceutics-16-01187-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/c60dc975196e/pharmaceutics-16-01187-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/9a6967dcb0bc/pharmaceutics-16-01187-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/589d1812e4d2/pharmaceutics-16-01187-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/be88c066cfda/pharmaceutics-16-01187-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50bd/11435238/dd41f9ad53c1/pharmaceutics-16-01187-g007.jpg

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Evaluation of a compounding phospholipid base for the percutaneous absorption of high molecular weight drugs using the Franz finite dose model.评价一种用于经皮吸收高分子量药物的复合磷脂基底的 Franz 有限剂量模型。
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Characteristics of a Lipid Hydrogel and Bigel as Matrices for Ascorbic Acid Stabilization.脂质水凝胶和双凝胶作为抗坏血酸稳定化基质的特性
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