School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, 510006, Guangdong, China.
Guangdong Provincial Key Laboratory of Advanced Drug Delivery, Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System, Guangdong Pharmaceutical University, Guangzhou, 510006, China.
J Fluoresc. 2024 Jul;34(4):1683-1692. doi: 10.1007/s10895-023-03385-y. Epub 2023 Aug 18.
In the present work, a simple and efficient stirring method was used to successfully synthesize a novel multifunctional carbon dots-drug delivery system AMP-CDs@5-Fu in the form of intertwined filaments. The results showed that AMP-CDs@5-Fu had the highest final release in the medium mimicking the physiological environment of the human small intestine compared to that of 5-Fu and that the drug release behaviors followed a zero-grade drug release within the first 3 h. The results also showed that AMP-CDs@5-Fu could be used to reduce the toxicity of 5-Fu while significantly improving the anticancer ability. In vitro hemolysis and anticancer assays showed that AMP-CDs@5-Fu could significantly improve the anticancer ability while decreasing the toxicity of 5-Fu, and the hemolysis rate of AMP-CDs@5-Fu was significantly lower than that of 5-Fu; their IC against 4T1 cancer cells were 201.63 ± 8.94 µg 5-Fu/mL and 241.24 ± 11.05 µg 5- Fu/mL. In addition, AMP-CDs@5-Fu allowed clear cell imaging. Therefore, AMP-CDs@5-Fu is expected to improve the bioavailability of 5-Fu as a novel oral agent with fluorescent properties and very promising as a novel fluorescence tracking drug loading system, which is expected to be used in the field of anticancer targeted therapy and fluorescence tracking to monitor the distribution of drugs.
在本工作中,采用简单高效的搅拌法成功合成了一种新型多功能碳点-药物传递系统 AMP-CDs@5-Fu,其形式为交织的纤维。结果表明,与 5-Fu 相比,在模拟人小肠生理环境的介质中,AMP-CDs@5-Fu 的最终释放量最高,药物释放行为在前 3 h 内遵循零级药物释放。结果还表明,AMP-CDs@5-Fu 可以降低 5-Fu 的毒性,同时显著提高抗癌能力。体外溶血和抗癌实验表明,AMP-CDs@5-Fu 可以显著提高抗癌能力,同时降低 5-Fu 的毒性,且 AMP-CDs@5-Fu 的溶血率明显低于 5-Fu;其对 4T1 癌细胞的 IC 分别为 201.63 ± 8.94 μg 5-Fu/mL 和 241.24 ± 11.05 μg 5-Fu/mL。此外,AMP-CDs@5-Fu 允许细胞清晰成像。因此,AMP-CDs@5-Fu 有望提高 5-Fu 的生物利用度,作为一种具有荧光特性的新型口服药物,并有望作为一种新型荧光跟踪药物载体系统,用于抗癌靶向治疗和荧光跟踪监测药物分布领域。