Department of Fundamental Chemistry, Laboratory of Supramolecular Chemistry & Nanotechnology, Institute of Chemistry, University of São Paulo, Avenida Professor Lineu Prestes, 748, São Paulo, São Paulo, 05508-000, Brazil.
Department of Clinical & Toxicological Analysis, Laboratory of Experimental Toxicology, Faculty of Pharmaceutical Sciences, University of São Paulo, Avenida Professor Lineu Prestes, 580, São Paulo, São Paulo, 05508-000, Brazil.
Nanomedicine (Lond). 2021 Apr;16(9):741-758. doi: 10.2217/nnm-2020-0459. Epub 2021 Apr 15.
The low solubility and consequent poor bioavailability of ibuprofen (IBU) is a major drawback that can be overcome by anchoring IBU on ultrasmall superparamagnetic iron oxide nanoparticles (USPIONs) as effective multifunctional carriers for drug delivery. USPIONs were conjugated with glycerol phosphate (USPION-GP) and also co-conjugated with IBU (USPION-GP/IBU), and their toxicity and anti-inflammatory effects investigated. Phosphate buffer saline (control), IBU, USPION-GP and USPION-GP/IBU were intravenously administered 15 min before lipopolysaccharide-induced peritonitis in male Balb/c mice. 4 h later, USPION bioconjugates did not appear to have caused toxicity to blood leukocytes or caused alterations in the spleen, liver or kidneys. Also, they inhibited lipopolysaccharide-induced neutrophil mobilization into the peritoneum. The absence of systemic toxicity and the unexpected anti-inflammatory action of USPION bioconjugates indicates that they could be a novel and effective approach to administer IBU and warrant further investigation.
布洛芬（IBU）的低溶解度和较差的生物利用度是一个主要的缺点，可以通过将 IBU 锚定在超顺磁性氧化铁纳米粒子（USPIONs）上来克服，将其作为药物输送的有效多功能载体。USPIONs 与甘油磷酸（USPION-GP）偶联，并且还与 IBU 共偶联（USPION-GP/IBU），并研究了它们的毒性和抗炎作用。磷酸盐缓冲盐水（对照）、IBU、USPION-GP 和 USPION-GP/IBU 在脂多糖诱导的雄性 Balb/c 小鼠腹膜炎前 15 分钟静脉给药。4 小时后，USPION 生物缀合物似乎没有引起血液白细胞毒性，也没有引起脾脏、肝脏或肾脏的改变。此外，它们抑制了脂多糖诱导的中性粒细胞向腹膜腔的迁移。USPION 生物缀合物没有全身毒性和意外的抗炎作用表明，它们可能是一种新型有效的给药方式，值得进一步研究。
