Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan.
Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan.
Int J Pharm. 2021 Dec 15;610:121255. doi: 10.1016/j.ijpharm.2021.121255. Epub 2021 Nov 1.
Curcumin (CUR) is a bioactive natural compound with potent antioxidant and anticancer properties. However, its poor water solubility has been a major limitation against its widespread clinical use. The aim of this study was to develop a nanoscale formulation for CUR to improve its solubility and potentially enhance its bioactivity, by leveraging the self-assembly behavior of tannic acid (TA) and amphiphilic poloxamers to form CUR-entrapped nanoassemblies. To optimize drug loading, formulation variables included the CUR: TA ratio and the type of amphiphilic polymer (Pluronic® F-127 or Pluronic® P-123). The optimal CUR nanoparticles (NPs) were around 200 nm in size with a high degree of monodispersity and 56% entrapment efficiency. Infrared spectroscopy confirmed the presence of intermolecular interactions between CUR and the NP formulation components. X-ray diffraction revealed that CUR was entrapped in the NPs in an amorphous state. The NPs maintained excellent colloidal stability under various conditions. In vitro release of CUR from the NPs showed a biphasic controlled release pattern up to 72 h. Antioxidant and antiproliferative assays against a panel of human cancer cell lines revealed significantly higher activity for CUR NPs compared to free CUR, particularly in MCF-7 and MDA-MB-231 breast cancer cells. This was attributed to greater cellular uptake of the NPs compared to the free drug as verified by confocal microscopy imaging and flow cytometry measurements. Our findings present a highly promising NP delivery platform for CUR prepared via a simple self-assembly process with the ability to potentiate its bioactivity in cancer and other diseases where oxidative stress is implicated.
姜黄素（CUR）是一种具有强大抗氧化和抗癌特性的生物活性天然化合物。然而，其较差的水溶性一直是其广泛临床应用的主要限制。本研究旨在通过利用鞣酸（TA）和两亲性泊洛沙姆的自组装行为来制备 CUR 纳米制剂，以提高其溶解度并可能增强其生物活性。为了优化药物载量，制剂变量包括 CUR：TA 比和两亲性聚合物的类型（Pluronic® F-127 或 Pluronic® P-123）。最佳 CUR 纳米粒子（NPs）的尺寸约为 200nm，具有高度的单分散性和 56%的包封效率。红外光谱证实了 CUR 与 NP 制剂成分之间存在分子间相互作用。X 射线衍射表明 CUR 以无定形状态包埋在 NPs 中。NP 在各种条件下均保持良好的胶体稳定性。从 NPs 中释放 CUR 的体外释放显示出长达 72h 的两相控制释放模式。对一系列人癌细胞系的抗氧化和抗增殖测定表明，与游离 CUR 相比，CUR NPs 的活性显著更高，特别是在 MCF-7 和 MDA-MB-231 乳腺癌细胞中。这归因于与游离药物相比，NP 具有更高的细胞摄取率，这通过共聚焦显微镜成像和流式细胞术测量得到了证实。我们的研究结果提出了一种很有前途的 CUR 纳米递药平台，该平台通过简单的自组装过程制备，具有增强其在涉及氧化应激的癌症和其他疾病中的生物活性的潜力。
