Chai Tiantian, Zhang Mengtong, Wang Shuo, Feng Jiankang, Feng Xibing, Shao Shihe, Lu Chichong, Jin Guofan
School of Pharmacy, Jiangsu University, Zhenjiang 212013, PR China.
Department of Gastroenterology, Yixing Hospital affiliated to Jiangsu University, Yixing 214200, PR China.
Int J Biol Macromol. 2025 Jan;284(Pt 1):137962. doi: 10.1016/j.ijbiomac.2024.137962. Epub 2024 Nov 26.
This study aims to construct a novel drug delivery strategy to address the poor bioavailability and biostability of curcumin. A curcumin delivery strategy, basing on post-polymerization modification of poly(2-vinyl-4,4-dimethyl azlactone) to obtain conjugates of curcumin and dendritic polymers, combined with sodium alginate coating is reported. The curcumin-polymer conjugates were shown to have good fluorescence properties with fluorescence quantum yields of 0.486 and 0.470, respectively. The composites were characterized as spherical nanoparticles with a desirable particle size of 221.7 nm and massive negatively charged surfaces. These aesthetic properties make it an acceptable drug delivery and release vehicle. In vitro release experiments showed that release of curcumin from the conjugates was controllable and acid-sensitive, which is expected to guide delivery targeting to cancer sites. In addition, biodistribution studies of the gastrointestinal tract of mice showed high levels of exposure. The results of cell imaging showed that conjugates have strong permeability to cancer cell membranes. They have been shown to have strong targeting and inhibitory effects on a variety of cancer cells, with an inhibition rate of up to about 90 %. Therefore, such novel vector designs show great potential in drug delivery mechanism research and cancer therapy.
本研究旨在构建一种新型药物递送策略,以解决姜黄素生物利用度低和生物稳定性差的问题。本文报道了一种基于聚(2-乙烯基-4,4-二甲基氮杂环丁烷)后聚合修饰以获得姜黄素与树枝状聚合物的共轭物,并结合海藻酸钠包衣的姜黄素递送策略。姜黄素-聚合物共轭物显示出良好的荧光特性,荧光量子产率分别为0.486和0.470。该复合材料被表征为球形纳米颗粒,粒径为221.7 nm,表面带大量负电荷。这些优良特性使其成为一种可接受的药物递送和释放载体。体外释放实验表明,姜黄素从共轭物中的释放是可控的且对酸敏感,有望引导药物靶向递送至癌症部位。此外,对小鼠胃肠道的生物分布研究显示其暴露水平较高。细胞成像结果表明,共轭物对癌细胞膜具有较强的渗透性。它们已被证明对多种癌细胞具有较强的靶向和抑制作用,抑制率高达约90%。因此,这种新型载体设计在药物递送机制研究和癌症治疗中显示出巨大潜力。