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硫酸亚铁粘膜黏附微球 - 治疗贫血口服铁剂的新方法。

Mucoadhesive microspheres of ferrous sulphate - A novel approach for oral iron delivery in treating anemia.

机构信息

Medical Devices Lab, Corporate R & D Centre, HLL Lifecare Ltd., Aakkulam, Sreekariyam. P.O. Thiruvananthapuram, 695 017, Kerala, India.

Diagnostics Lab, Corporate R & D Centre, HLL Lifecare Ltd., Aakkulam, Sreekariyam. P.O. Thiruvananthapuram, 695 017, Kerala, India.

出版信息

Colloids Surf B Biointerfaces. 2020 Nov;195:111247. doi: 10.1016/j.colsurfb.2020.111247. Epub 2020 Jul 8.

Abstract

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.

摘要

硫酸亚铁是一种广泛应用的口服铁补充剂,但其生物利用度低,副作用大。在这项研究中,我们采用喷雾干燥技术,将硫酸亚铁用高黏液附着性聚合物(如羟丙基甲基纤维素(HP)、壳聚糖(CS)和卡波姆(CP))进行包衣,制备具有良好产率和高包封效率的黏液附着性聚合物包衣微球。黏液附着性包衣可能使这些微球附着在肠道上,从而提高硫酸亚铁的吸收效果。体外释放研究表明,微球的释放遵循非 Fickian 零级药物释放规律。CP 和 CSHP 包衣微球表现出良好的溶胀(∼1200 至 2400%)和黏液附着性能(58-95%),表明与游离硫酸亚铁相比,它们可以膨胀并附着在肠道上更长时间。所有微球在 Caco2 细胞系和成纤维细胞系中均表现出非细胞毒性。在 Caco2 细胞系上进行的细胞摄取研究表明,与游离硫酸亚铁相比,载有硫酸亚铁的微球向细胞内的摄取增加且释放更持久。尽管细胞摄取研究显示硫酸亚铁微球的摄取增加,但在给予苯肼诱导贫血大鼠时,硫酸亚铁微球和硫酸亚铁的疗效相当。

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