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用于多酚递送系统的金属藻酸盐:关于交联离子及用于皮肤中保护性黄酮类化合物释放的易用型贴剂的研究。

Metal alginates for polyphenol delivery systems: Studies on crosslinking ions and easy-to-use patches for release of protective flavonoids in skin.

作者信息

Silva João, Vanat Pavlo, Marques-da-Silva Dorinda, Rodrigues Joaquim Rui, Lagoa Ricardo

机构信息

School of Technology and Management, Polytechnic Institute of Leiria, Portugal.

Laboratório Associado LSRE-LCM, School of Technology and Management, Polytechnic Institute of Leiria, Portugal.

出版信息

Bioact Mater. 2020 Apr 6;5(3):447-457. doi: 10.1016/j.bioactmat.2020.03.012. eCollection 2020 Sep.

Abstract

Incorporation of bioactive natural compounds like polyphenols is an attractive approach for enhanced functionalities of biomaterials. In particular flavonoids have important pharmacological activities, and controlled release systems may be instrumental to realize the full potential of these phytochemicals. Alginate presents interesting attributes for dermal and other biomaterial applications, and studies were carried here to support the development of polyphenol-loaded alginate systems. Studies of capillary viscosity indicated that ionic medium is an effective strategy to modulate the polyelectrolyte effect and viscosity properties of alginates. On gelation, considerable differences were observed between alginate gels produced with Ca, Ba, Cu, Fe, Fe and Zn as crosslinkers, especially concerning shrinkage and morphological regularity. Stability assays with different polyphenols in the presence of alginate-gelling cations pointed to the choice of calcium, barium and zinc as safer crosslinkers. Alginate-based films loaded with epicatechin were prepared and the kinetics of release of the flavonoid investigated. The results with calcium, barium and zinc alginate matrices indicated that the release dynamics is dependent on film thicknesses, but also on the crosslinking metal used. On these grounds, an alginate-based system of convenient use was devised, so that flavonoids can be easily loaded at simple point-of-care conditions before dermal application. This epicatechin-loaded patch was tested on an skin model and demonstrated capacity to deliver therapeutically relevant concentrations on skin surface. Moreover, the flavonoid released was not modified and retained full antioxidant bioactivity. The alginate-based system proposed offers a multifunctional approach for flavonoid controllable delivery and protection of skin injured or under risk.

摘要

将生物活性天然化合物(如多酚)掺入生物材料中是增强其功能的一种有吸引力的方法。特别是黄酮类化合物具有重要的药理活性,而控释系统可能有助于充分发挥这些植物化学物质的潜力。藻酸盐在皮肤和其他生物材料应用中具有有趣的特性,在此进行了相关研究以支持负载多酚的藻酸盐系统的开发。毛细管粘度研究表明,离子介质是调节藻酸盐的聚电解质效应和粘度特性的有效策略。在凝胶化过程中,观察到以钙、钡、铜、铁、铁和锌作为交联剂制备的藻酸盐凝胶之间存在显著差异,特别是在收缩和形态规则性方面。在藻酸盐凝胶化阳离子存在下对不同多酚进行的稳定性测定表明,选择钙、钡和锌作为更安全的交联剂。制备了负载表儿茶素的藻酸盐基薄膜,并研究了黄酮类化合物的释放动力学。钙、钡和锌藻酸盐基质的结果表明,释放动力学不仅取决于薄膜厚度,还取决于所使用的交联金属。基于这些理由,设计了一种使用方便的藻酸盐基系统,以便在皮肤应用前的简单即时护理条件下轻松负载黄酮类化合物。在皮肤模型上测试了这种负载表儿茶素的贴片,结果表明其能够在皮肤表面递送具有治疗相关性的浓度。此外,释放的黄酮类化合物未被改性并保留了全部抗氧化生物活性。所提出的基于藻酸盐的系统为黄酮类化合物的可控递送以及对受伤或处于风险中的皮肤的保护提供了一种多功能方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5184/7139165/94864ca1fe7b/gr2.jpg

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