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姜黄素载药及共载纳米系统:从增强生物学活性角度的综述。

Curcumin Loaded and Co-loaded Nanosystems: A Review from a Biological Activity Enhancement Perspective.

机构信息

Laboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE, 1174-1200, Pavas, San José, Costa Rica.

Laboratorio de Antioxidantes y Alimentos Funcionales, Centro de Investigación en Alimentación y Desarrollo (CIAD), A.C., Carretera Gustavo Enrique Astiazarán Rosas No. 46, Col. La Victoria, Hermosillo, Sonora 83304, Mexico.

出版信息

Pharm Nanotechnol. 2021;9(2):85-100. doi: 10.2174/2211738508666201228150659.

Abstract

BACKGROUND

Curcumin is a natural phenolic compound exhibiting multiple bioactivities that have been evaluated in vitro, in vivo as well as through clinical studies in humans. Some of them include antimicrobial, antioxidant, anti-inflammatory, and central nervous system protective effects. Further, curcumin is generally recognized as a safe substance because of its low toxicity. However, its molecular structure is susceptible to changes in pH, oxidation, photodegradation, low aqueous solubility, and biotransformation compromising its bioavailability; these drawbacks are successfully addressed through nanotechnology.

OBJECTIVE

The present review systematizes findings on the enhancement of curcumin's beneficial effects when it is loaded and co-loaded into different types of nanosystems covering liposomes, polymeric and solid-lipid nanoparticles, nanostructured lipid carrier, lipid-polymeric hybrids, self- -assembled and protein-based core-shell systems in relation to its antimicrobial, antioxidant, anti-inflammatory and central nervous system protective bioactivities.

CONCLUSION

Curcumin is a versatile molecule capable of exerting antimicrobial, antioxidant, anti- inflammatory, and central nervous system protective effects in an enhanced manner using the possibilities offered by the nanotechnology-based approach. Its enhanced bioactivities are associated with increments in solubility, stability, bioavailability, as well as in improved intracellular uptake and cell internalization. These advantages, in addition to curcumin's low toxicity, indicate the potential of curcumin to be loaded and co-loaded into nanosystems capable of providing a controlled release and targeted administration.

摘要

背景

姜黄素是一种天然酚类化合物,具有多种生物活性,已在体外、体内以及人体临床研究中进行了评估。其中一些包括抗菌、抗氧化、抗炎和中枢神经系统保护作用。此外,由于其毒性低,姜黄素通常被认为是一种安全的物质。然而,其分子结构容易受到 pH 值变化、氧化、光降解、低水溶性和生物转化的影响,从而降低其生物利用度;这些缺点可以通过纳米技术成功解决。

目的

本综述系统地总结了将姜黄素负载和共负载到不同类型的纳米系统中时,增强其有益作用的研究结果,这些纳米系统包括脂质体、聚合物和固体脂质纳米粒、纳米结构脂质载体、脂质-聚合物杂化物、自组装和基于蛋白质的核壳系统,涉及到其抗菌、抗氧化、抗炎和中枢神经系统保护的生物活性。

结论

姜黄素是一种多功能分子,能够通过利用基于纳米技术的方法提供的可能性,以增强的方式发挥抗菌、抗氧化、抗炎和中枢神经系统保护作用。其增强的生物活性与溶解度、稳定性、生物利用度的提高以及细胞内摄取和细胞内化的改善有关。除了姜黄素的低毒性外,这些优势表明将姜黄素负载和共负载到能够提供控制释放和靶向给药的纳米系统中具有潜力。

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