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基于原生素纳米载体的天然抗氧化和光保护化合物在蜂胶中的递释系统:一种改善其在生物相关介质中的溶解行为和皮肤滞留特性的方法。

Phytosomal nanocarriers as platforms for improved delivery of natural antioxidant and photoprotective compounds in propolis: An approach for enhanced both dissolution behaviour in biorelevant media and skin retention profiles.

机构信息

School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK; Department of Pharmaceutics, Faculty of Pharmacy, Hasanuddin University, Makassar, Indonesia.

College of Pharmacy STIFA Kebangsaan, Makassar, Indonesia.

出版信息

J Photochem Photobiol B. 2020 Apr;205:111846. doi: 10.1016/j.jphotobiol.2020.111846. Epub 2020 Mar 2.

DOI:10.1016/j.jphotobiol.2020.111846
PMID:32151785
Abstract

Propolis has been reported to possess rich content of antioxidant compounds and may provide health benefits through oxidative stress reduction. Presently, the formulation activities used to enhance the drug delivery have been hampered due to inherently low aqueous solubility and poor transdermal permeation of the bioactive phenols and flavonoids. Here, we show, the formulation of propolis extract (PE) into phytosome delivery systems. The optimum antioxidant activity was attained through extraction process using 75% v/v ethanol. The phytosome was prepared using thin-layer hydration technique with l-α-Phosphatidylcholine as a phospholipid. Fourier transform infrared (FTIR) was used to investigate the occurrence of molecular interactions between formulation components. This innovative approach could encapsulate >40% of bioactive compounds in PE, namely caffeic acid, quercetin, and kaempferol. FTIR spectroscopy indicated new hydrogen bond formation, supporting successful phytosome formulation. The phytosomes enhanced the dissolution up to 4-folds of bioactive compounds in bio-mimicked release media, as well as improved penetrability and skin retention up to 6-folds of the three main compounds of propolis, when compared to non-encapsulated PE formulation. Importantly, the hydrogel containing phytosome showed a potential for UVA and UVB radiation absorption, indicated by the SPF values of higher than 15. To conclude, this work shows promising novel delivery approaches for PE in the treatment of organ injured stress oxidative and skin aging.

摘要

蜂胶被报道含有丰富的抗氧化化合物,可通过减少氧化应激提供健康益处。目前,由于生物活性酚类和类黄酮的固有低水溶解度和差的透皮渗透,用于增强药物递送的制剂活性受到阻碍。在这里,我们展示了将蜂胶提取物 (PE) 制成植物甾醇递送系统。通过使用 75% v/v 乙醇的提取过程达到最佳抗氧化活性。植物甾醇是使用薄层水合技术用 l-α-磷脂酰胆碱作为磷脂制备的。傅里叶变换红外 (FTIR) 用于研究制剂成分之间分子相互作用的发生。这种创新方法可以将>40%的 PE 中的生物活性化合物,即咖啡酸、槲皮素和山奈酚包封在内。FTIR 光谱表明形成了新的氢键,支持成功的植物甾醇制剂。与非包封的 PE 制剂相比,植物甾醇增强了生物模拟释放介质中生物活性化合物的溶解度高达 4 倍,以及提高了蜂胶中三种主要化合物的透皮性和皮肤滞留性高达 6 倍。重要的是,含有植物甾醇的水凝胶显示出吸收 UVA 和 UVB 辐射的潜力,这表明 SPF 值高于 15。总之,这项工作展示了治疗器官损伤应激氧化和皮肤老化的 PE 的有前途的新型递送方法。

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