Department of Environmental Science and Policy, Università degli Studi di Milano, Via Celoria 2, 20133 Milano, Italy.
Department of Biosciences, Università degli Studi di Milano, Via Celoria 26, 20133 Milano, Italy.
Molecules. 2022 Oct 18;27(20):6997. doi: 10.3390/molecules27206997.
The research for alternative administration methods for anticancer drugs, towards enhanced effectiveness and selectivity, represents a major challenge for the scientific community. In the last decade, polymeric nanostructured delivery systems represented a promising alternative to conventional drug administration since they ensure secure transport to the selected target, providing active compounds protection against elimination, while minimizing drug toxicity to non-target cells. In the present research, poly(glycerol sebacate), a biocompatible polymer, was synthesized and then nanostructured to allow curcumin encapsulation, a naturally occurring polyphenolic phytochemical isolated from the powdered rhizome of L. Curcumin was selected as an anticancer agent in virtue of its strong chemotherapeutic activity against different cancer types combined with good cytocompatibility within healthy cells. Despite its strong and fascinating biological activity, its possible exploitation as a novel chemotherapeutic has been hampered by its low water solubility, which results in poor absorption and low bioavailability upon oral administration. Hence, its encapsulation within nanoparticles may overcome such issues. Nanoparticles obtained through nanoprecipitation, an easy and scalable technique, were characterized in terms of size and stability over time using dynamic light scattering and transmission electron microscopy, confirming their nanosized dimensions and spherical shape. Finally, biological investigation demonstrated an enhanced cytotoxic effect of curcumin-loaded PGS-NPs on human cervical cancer cells compared to free curcumin.
研究用于抗癌药物的替代给药方法,以提高疗效和选择性,是科学界面临的重大挑战。在过去的十年中,聚合物流体纳米给药系统作为传统药物给药的替代方法具有广阔的应用前景,因为它们能够确保药物安全地输送到靶部位,保护活性化合物免受清除,同时将药物对非靶细胞的毒性降至最低。在本研究中,合成了生物相容性聚合物聚(癸二酸甘油酯)(poly(glycerol sebacate)),然后对其进行纳米结构化处理以封装姜黄素(curcumin)。姜黄素是一种天然存在的多酚类植物化学物质,从 L. 的粉末状根茎中分离出来。姜黄素具有很强的针对不同癌症类型的化学治疗活性,并且在健康细胞中具有良好的细胞相容性,因此被选为抗癌药物。尽管其具有很强的吸引人的生物活性,但由于其低水溶性,导致口服吸收差,生物利用度低,其作为新型化学治疗药物的开发受到了阻碍。因此,将其封装在纳米颗粒中可能会克服这些问题。通过简单且可扩展的纳米沉淀技术获得的纳米颗粒,通过动态光散射和透射电子显微镜对其尺寸和随时间的稳定性进行了表征,证实了其纳米级尺寸和球形形状。最后,生物学研究表明,与游离姜黄素相比,负载姜黄素的 PGS-NPs 对人宫颈癌细胞具有增强的细胞毒性作用。