聚乙烯吡咯烷酮修饰纳米硒在大鼠体内的生物安全性及药代动力学特征。

OBJECTIVE: This study aims to investigate the biocompatibility and pharmacokinetic characteristics of polyvinyl pyrrolidone-modified selenium nanoparticles (PVP-Se NPs). Understanding the biosafety of PVP-Se NPs is crucial due to their potential applications in mitigating oxidative stress-related diseases and improving drug delivery systems. METHODS: Selenium nanoparticles were prepared using a sodium selenite solution, followed by PVP modification. Particle size analysis was conducted using dynamic light scattering (DLS), and particle morphology was observed using transmission electron microscopy (TEM). Different concentrations of PVP-Se NPs were intraperitoneally injected into SD rats, and the survival rate was observed. Liver and kidney tissues, urine, feces, and blood samples were collected at the highest safe dose, and the concentration of selenium ions was measured. RESULTS: The average particle size of PVP-Se NPs was 278.4 ± 124.8 nm, exhibiting a semi-spherical shape. The maximum safe dose of PVP-Se NPs for intraperitoneal injection in rats was approximately 320 µg/kg. At this dose, the content of PVP-Se NPs significantly increased in the liver and kidney tissues from day 1 to day 3, in urine and feces during the first 8 h, and in blood during the first 2 h, followed by a gradual decrease. CONCLUSION: When administered at a safe dose, PVP-Se NPs do not damage liver and kidney tissues and can be eliminated from the body through liver and kidney metabolism without accumulation.

目的：本研究旨在探讨聚乙烯吡咯烷酮（PVP）修饰的硒纳米粒子（PVP-Se NPs）的生物相容性和药代动力学特征。由于 PVP-Se NPs 在缓解氧化应激相关疾病和改善药物传递系统方面具有潜在应用，因此了解其生物安全性至关重要。

方法：使用亚硒酸钠溶液制备硒纳米粒子，然后进行 PVP 修饰。使用动态光散射（DLS）进行粒径分析，使用透射电子显微镜（TEM）观察颗粒形态。将不同浓度的 PVP-Se NPs 腹腔注射到 SD 大鼠中，观察存活率。在最高安全剂量下收集肝和肾组织、尿液、粪便和血液样本，并测量硒离子浓度。

结果：PVP-Se NPs 的平均粒径为 278.4 ± 124.8nm，呈半球形。PVP-Se NPs 腹腔注射大鼠的最大安全剂量约为 320μg/kg。在此剂量下，PVP-Se NPs 在第 1 天至第 3 天在肝和肾组织中的含量显著增加，在第 1 天至第 8 小时在尿液和粪便中的含量增加，在第 1 天至第 2 小时在血液中的含量增加，随后逐渐减少。

结论：在安全剂量下给药时，PVP-Se NPs 不会损伤肝和肾组织，并可通过肝和肾代谢从体内消除，不会积累。