Department of Pharmaceutics, I.S.F. College of Pharmacy, Moga, Punjab, India.
Department of Pharmaceutics, I.S.F. College of Pharmacy, Moga, Punjab, India.
J Pharm Sci. 2018 Oct;107(10):2663-2673. doi: 10.1016/j.xphs.2018.06.014. Epub 2018 Jun 21.
The objective of the present study is to improve iron bioavailability using high-density gastroretentive pellets of zero valent iron nanoparticles (ZVINPs). ZVINPs were prepared by the chemical reduction method and were characterized for surface morphology, surface charge, and thermal properties. High-density gastroretentive pellets of iron nanoparticles were prepared using spheronization technique. Pellets were characterized for its micromeritic properties, in vitro drug release, and ex vivo permeability. The pharmacokinetic parameters, organ distribution, and toxicity of the optimized pellets were investigated in Wistar rats. In vivo results revealed more than 2-fold increases in oral bioavailability of iron by pellets compared to plane ferrous sulfate. Toxicological studies of the carriers indicated no evidence of liver damage in acute treatment; however, few complications were observed in chronic treatment groups. These results indicated that ZVINPs pellets successfully improve the oral iron bioavailability but need to obtain more information on repeated dose toxicity to initiate the clinical evaluation of investigational products.
本研究的目的是通过使用零价铁纳米粒子（ZVINPs）高密度胃滞留微丸来提高铁的生物利用度。ZVINPs 通过化学还原法制备，并对其表面形态、表面电荷和热性能进行了表征。使用球形化技术制备了高密度胃滞留铁纳米粒子微丸。对微丸的微粉特性、体外药物释放和离体渗透性进行了表征。在 Wistar 大鼠中研究了优化微丸的药代动力学参数、器官分布和毒性。体内结果表明，与普通硫酸亚铁相比，微丸使铁的口服生物利用度提高了 2 倍以上。载体的毒理学研究表明，急性治疗中没有肝脏损伤的证据；然而，在慢性治疗组中观察到一些并发症。这些结果表明，ZVINPs 微丸成功地提高了口服铁的生物利用度，但需要获得更多关于重复剂量毒性的信息，以启动对研究产品的临床评估。
