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负载铁的固体脂质纳米粒克服缺铁性贫血治疗障碍

Solid lipid nanoparticles loaded with iron to overcome barriers for treatment of iron deficiency anemia.

作者信息

Hosny Khaled Mohamed, Banjar Zainy Mohammed, Hariri Amani H, Hassan Ali Habiballah

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia ; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni Suef University, Beni Suef, Egypt.

Department of Clinical Biochemistry, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia.

出版信息

Drug Des Devel Ther. 2015 Jan 8;9:313-20. doi: 10.2147/DDDT.S77702. eCollection 2015.

Abstract

According to the World Health Organization, 46% of the world's children suffer from anemia, which is usually treated with iron supplements such as ferrous sulfate. The aim of this study was to prepare iron as solid lipid nanoparticles, in order to find an innovative way for alleviating the disadvantages associated with commercially available tablets. These limitations include adverse effects on the digestive system resulting in constipation and blood in the stool. The second drawback is the high variability in the absorption of iron and thus in its bioavailability. Iron solid lipid nanoparticles (Fe-SLNs) were prepared by hot homogenization/ultrasonication. Solubility of ferrous sulfate in different solid lipids was measured, and effects of process variables such as the surfactant type and concentration, homogenization and ultrasonication times, and charge-inducing agent on the particle size, zeta potential, and encapsulation efficiency were determined. Furthermore, in vitro drug release and in vivo pharmacokinetics were studied in rabbits. Results indicated that Fe-SLNs consisted of 3% Compritol 888 ATO, 1% Lecithin, 3% Poloxamer 188, and 0.2% dicetylphosphate, with an average particle size of 25 nm with 92.3% entrapment efficiency. In vivo pharmacokinetic study revealed more than fourfold enhanced bioavailability. In conclusion, Fe-SLNs could be a promising carrier for iron with enhanced oral bioavailability.

摘要

根据世界卫生组织的数据,全球46%的儿童患有贫血症,通常用硫酸亚铁等铁补充剂进行治疗。本研究的目的是制备铁固体脂质纳米粒,以找到一种创新方法来缓解市售片剂的缺点。这些局限性包括对消化系统产生不良影响,导致便秘和便血。第二个缺点是铁的吸收以及生物利用度存在很大差异。通过热均质化/超声处理制备了铁固体脂质纳米粒(Fe-SLNs)。测定了硫酸亚铁在不同固体脂质中的溶解度,并确定了表面活性剂类型和浓度、均质化和超声处理时间以及电荷诱导剂等工艺变量对粒径、zeta电位和包封率的影响。此外,还对家兔进行了体外药物释放和体内药代动力学研究。结果表明,Fe-SLNs由3%的Compritol 888 ATO、1%的卵磷脂、3%的泊洛沙姆188和0.2%的十六烷基磷酸酯组成,平均粒径为25 nm,包封率为92.3%。体内药代动力学研究表明生物利用度提高了四倍多。总之,Fe-SLNs可能是一种有前途的铁载体,具有提高的口服生物利用度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57eb/4293289/5dd67f5e27f1/dddt-9-313Fig1.jpg

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