Silvestre Fernanda, Santos Carolina, Silva Vitória, Ombredane Alicia, Pinheiro Willie, Andrade Laise, Garcia Mônica, Pacheco Thyago, Joanitti Graziella, Luz Glécia, Carneiro Marcella
Laboratory of Bioactive Compounds and Nanobiotechnology (LCBNano), Campus Darcy Ribeiro, University of Brasilia, Brasilia 70910-900, Brazil.
Post-Graduate Program in Nanoscience and Nanobiotechnology, Institute of Biological Sciences, Campus Darcy Ribeiro, University of Brasilia, Brasilia 70910-900, Brazil.
Pharmaceuticals (Basel). 2023 Jun 29;16(7):943. doi: 10.3390/ph16070943.
Curcumin is a polyphenolic compound, derived from Curcuma longa, and it has several pharmacological effects such as antioxidant, anti-inflammatory, and antitumor. Although it is a pleiotropic molecule, curcumin's free form, which is lipophilic, has low bioavailability and is rapidly metabolized, limiting its clinical use. With the advances in techniques for loading curcumin into nanostructures, it is possible to improve its bioavailability and extend its applications. In this review, we gather evidence about the comparison of the pharmacokinetics (biodistribution and bioavailability) between free curcumin (Cur) and nanostructured curcumin (Cur-NPs) and their respective relationships with antitumor efficacy. The search was performed in the following databases: Cochrane, LILACS, Embase, MEDLINE/Pubmed, Clinical Trials, BSV regional portal, ScienceDirect, Scopus, and Web of Science. The selected studies were based on studies that used High-Performance Liquid Chromatography (HPLC) as the pharmacokinetics evaluation method. Of the 345 studies initially pooled, 11 met the inclusion criteria and all included studies classified as high quality. In this search, a variety of nanoparticles used to deliver curcumin (polymeric, copolymeric, nanocrystals, nanovesicles, and nanosuspension) were found. Most Cur-NPs presented negative Zeta potential ranging from -25 mV to 12.7 mV, polydispersion index (PDI) ranging from 0.06 to 0.283, and hydrodynamic diameter ranging from 30.47 to 550.1 nm. Selected studies adopted mainly oral and intravenous administrations. In the pharmacokinetics analysis, samples of plasma, liver, tumor, lung, brain, kidney, and spleen were evaluated. The administration of curcumin, in nanoparticle systems, resulted in a higher level of curcumin in tumors compared to free curcumin, leading to an improved antitumor effect. Thus, the use of nanoparticles can be a promising alternative for curcumin delivery since this improves its bioavailability.
姜黄素是一种源自姜黄的多酚类化合物，具有抗氧化、抗炎和抗肿瘤等多种药理作用。尽管姜黄素是一种具有多种功能的分子，但其亲脂性的游离形式生物利用度低且代谢迅速，限制了其临床应用。随着将姜黄素负载到纳米结构中的技术进步，提高其生物利用度并扩展其应用成为可能。在本综述中，我们收集了有关游离姜黄素（Cur）和纳米结构姜黄素（Cur-NPs）之间药代动力学（生物分布和生物利用度）比较以及它们与抗肿瘤疗效各自关系的证据。检索在以下数据库中进行：Cochrane、LILACS、Embase、MEDLINE/Pubmed、临床试验、BSV区域门户、ScienceDirect、Scopus和Web of Science。所选研究基于使用高效液相色谱（HPLC）作为药代动力学评估方法的研究。在最初汇总的345项研究中，11项符合纳入标准，所有纳入研究均被归类为高质量。在此次检索中，发现了多种用于递送姜黄素的纳米颗粒（聚合物、共聚物、纳米晶体、纳米囊泡和纳米悬浮液）。大多数Cur-NPs的zeta电位为负，范围在-25 mV至12.7 mV之间，多分散指数（PDI）范围在0.06至0.283之间，流体动力学直径范围在30.47至550.1 nm之间。所选研究主要采用口服和静脉给药。在药代动力学分析中，对血浆、肝脏、肿瘤、肺、脑、肾和脾脏样本进行了评估。与游离姜黄素相比，在纳米颗粒系统中给予姜黄素导致肿瘤中姜黄素水平更高，从而提高了抗肿瘤效果。因此，使用纳米颗粒可能是递送姜黄素的一种有前景的替代方法，因为这提高了其生物利用度。
