Laboratório de Planejamento e Desenvolvimento de Fármacos, Instituto de Ciências Exatas e Naturais, Universidade Federal do Pará, Belem 66075-110, Pará, Brazil.
Microbiology Laboratory, Faculty of Pharmacy, Federal University of Pará, Belem 66075-110, Pará, Brazil.
Molecules. 2023 Jun 24;28(13):4973. doi: 10.3390/molecules28134973.
Caffeic acid (CA) exhibits a myriad of biological activities including cardioprotective action, antioxidant, antitumor, anti-inflammatory, and antimicrobial properties. On the other hand, CA presents low water solubility and poor bioavailability, which have limited its use for therapeutic applications. The objective of this study was to develop a nanohybrid of zinc basic salts (ZBS) and chitosan (Ch) containing CA (ZBS-CA/Ch) and evaluate its anti-edematogenic and antioxidant activity in dextran and carrageenan-induced paw edema model. The samples were obtained by coprecipitation method and characterized by X-ray diffraction, Fourier transform infrared (FT-IR), scanning electron microscope (SEM) and UV-visible spectroscopy. The release of caffeate anions from ZBS-CA and ZBS-CA/Ch is pH-dependent and is explained by a pseudo-second order kinetics model, with a linear correlation coefficient of R ≥ 0.99 at pH 4.8 and 7.4. The in vivo pharmacological assays showed excellent anti-edematogenic and antioxidant action of the ZBS-CA/Ch nanoparticle with slowly releases of caffeate anions in the tissue, leading to a prolongation of CA-induced anti-edematogenic and anti-inflammatory activities, as well as improving its inhibition or sequestration antioxidant action toward reactive species. Overall, this study highlighted the importance of ZBS-CA/Ch as an optimal drug carrier.
咖啡酸(CA)具有多种生物学活性,包括心脏保护作用、抗氧化、抗肿瘤、抗炎和抗菌特性。另一方面,CA 的水溶性低,生物利用度差,这限制了它在治疗应用中的使用。本研究的目的是开发一种含有 CA 的锌碱盐(ZBS)和壳聚糖(Ch)的纳米杂化体(ZBS-CA/Ch),并评估其在葡聚糖和角叉菜胶诱导的爪肿胀模型中的抗水肿和抗氧化活性。样品通过共沉淀法获得,并通过 X 射线衍射、傅里叶变换红外(FT-IR)、扫描电子显微镜(SEM)和紫外可见光谱进行表征。ZBS-CA 和 ZBS-CA/Ch 中咖啡酸阴离子的释放是 pH 依赖性的,并通过拟二级动力学模型解释,在 pH 4.8 和 7.4 时线性相关系数 R ≥ 0.99。体内药理试验表明,ZBS-CA/Ch 纳米粒子具有优异的抗水肿和抗氧化作用,在组织中缓慢释放咖啡酸阴离子,从而延长 CA 诱导的抗水肿和抗炎作用,并提高其对活性物质的抑制或捕获抗氧化作用。总的来说,这项研究强调了 ZBS-CA/Ch 作为一种理想药物载体的重要性。