Deng Dezhi, Zhang Rong, Wu Jiaoxia, Wang Lisha, Zhang Qiaoling, Zhang Junqing, Tan Yinfeng, Chen Kai, Li Yonghui
Key Laboratory of Tropical Translational Medicine of Ministry of Education, Hainan Provincial Key Laboratory of Research and Development on Tropical Herbs, Haikou Key Laboratory of Li Nationality Medicine, School of Pharmacy, Hainan Medical University, Haikou 571199, China.
Key Laboratory of Tropical Translational Medicine of Ministry of Education, Hainan Provincial Key Laboratory of Research and Development on Tropical Herbs, Haikou Key Laboratory of Li Nationality Medicine, School of Pharmacy, Hainan Medical University, Haikou 571199, China.
Int J Biol Macromol. 2025 Mar;292:139367. doi: 10.1016/j.ijbiomac.2024.139367. Epub 2024 Dec 30.
The use of natural polysaccharides from traditional Chinese medicine as carrier materials has great potentiality in drug delivery. Nootkatone (NKT) demonstrated good pharmacological activity in treating kidney injury, but its solubility and bioavailability are not very good which may affect the effectiveness of its therapeutic effect. Alpinia oxyphylla fructus polysaccharide (AOP), as a plant polysaccharide, has multiple pharmacological activities and may help to provide synergy for NKT. Therefore, AOP nanoparticles loaded with NKT (AOP-NKT NPs) were prepared for the prevention of acute kidney injury in this study. The sizes of AOP-NKT NPs are 291.60 ± 3.73 nm, and the Zeta potential values are 35.2 ± 0.65 mV. The nanoparticles exhibited excellent stability in pH, NaCl solution, temperature, and storage. The nanoparticles also improved the solubility and oral bioavailability of NKT. In biocompatibility experiments, AOP-NKT NPs showed lower macrophage toxicity than NKT, and the nanoparticles had good blood compatibility and in vivo biosafety. In vivo, prophylactic administration of this nanoparticle could enhance the ability of NKT in promoting macrophage M2 polarization, reducing renal inflammation and thus improve renal function and repair renal damage. In conclusion, the present study may provide the possibility for AOP as a nano delivery vehicle for renal injury protective drugs.
将来自中药的天然多糖用作载体材料在药物递送方面具有巨大潜力。诺卡酮（NKT）在治疗肾损伤方面显示出良好的药理活性，但其溶解度和生物利用度不太理想，这可能会影响其治疗效果的有效性。益智仁多糖（AOP）作为一种植物多糖，具有多种药理活性，可能有助于为NKT提供协同作用。因此，本研究制备了负载NKT的AOP纳米颗粒（AOP-NKT NPs）用于预防急性肾损伤。AOP-NKT NPs的粒径为291.60 ± 3.73 nm，Zeta电位值为35.2 ± 0.65 mV。这些纳米颗粒在pH值、氯化钠溶液、温度和储存条件下表现出优异的稳定性。纳米颗粒还提高了NKT的溶解度和口服生物利用度。在生物相容性实验中，AOP-NKT NPs显示出比NKT更低的巨噬细胞毒性，并且纳米颗粒具有良好的血液相容性和体内生物安全性。在体内，预防性给予这种纳米颗粒可以增强NKT促进巨噬细胞M2极化、减轻肾脏炎症的能力，从而改善肾功能并修复肾脏损伤。总之，本研究可能为AOP作为肾损伤保护药物的纳米递送载体提供可能性。
