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Mucoadhesive microspheres of ferrous sulphate - A novel approach for oral iron delivery in treating anemia.
Colloids and Surfaces B: Biointerfaces ( IF 5.4 ) Pub Date : 2020-07-08 , DOI: 10.1016/j.colsurfb.2020.111247
Rahul B S 1 , Lakshmi S 2 , Sneha Letha S 1 , Sidharth Mohan M 1 , Rosemary M J 1
Affiliation  

Ferrous sulphate is a widely used oral iron supplement with low bioavailability and substantial side effects. In this study ferrous sulphate has been coated with highly mucoadhesive polymers such as hydroxypropylmethyl cellulose (HP), chitosan (CS) and carbopol (CP) by spray drying technique to produce mucoadhesive polymer coated microspheres with good yield and high encapsulation efficiency. Mucoadhesive coating may allow these microspheres to get attached to the intestine and hence better absorption of ferrous sulphate may be achieved. in vitro release studies from the microspheres show that the release follows non-Fickian zero order drug release. CP and CSHP coated microspheres showed good swelling(∼1200 to 2400 %) and mucoadhesion properties (58–95 %) indicating that they can swell and get attached to the intestine for longer time period as compared to free ferrous sulphate. All the microspheres were found to be non-cytotoxic in Caco2 cell lines and fibroblast cell lines. Cell uptake studies conducted on Caco2 cell lines showed that uptake of microspheres containing ferrous sulphate has an increased and sustained release to the cell as compared to free ferrous sulphate. Though cell uptake studies showed an increase in uptake for ferrous sulphate microspheres, comparable efficacy was observed upon administering ferrous sulphate microspheres and ferrous sulphate to phenyl hydrazine induced anemic rats.



中文翻译:

硫酸亚铁的粘膜粘附微球 - 一种口服铁剂治疗贫血的新方法。

硫酸亚铁是一种广泛使用的口服铁补充剂,具有低生物利用度和大量副作用。在这项研究中,硫酸亚铁通过喷雾干燥技术包覆了高黏膜粘附聚合物,如羟丙基甲基纤维素 (HP)、壳聚糖 (CS) 和卡波姆 (CP),以生产具有良好收率和高封装效率的黏膜粘附聚合物包覆微球。粘膜粘附涂层可以让这些微球附着在肠道上,因此可以更好地吸收硫酸亚铁。体外来自微球的释放研究表明释放遵循非菲克零级药物释放。CP 和 CSHP 涂层的微球显示出良好的溶胀性(~1200% 至 2400%)和粘膜粘附特性​​(58-95%),表明与游离硫酸亚铁相比,它们可以溶胀并附着在肠道上的时间更长。发现所有微球在 Caco2 细胞系和成纤维细胞系中均无细胞毒性。对 Caco2 细胞系进行的细胞摄取研究表明,与游离硫酸亚铁相比,含有硫酸亚铁的微球的摄取增加并持续释放到细胞中。尽管细胞摄取研究显示硫酸亚铁微球的摄取增加,

更新日期:2020-07-22
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