Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.
Ther Deliv. 2021 Apr;12(4):297-310. doi: 10.4155/tde-2020-0123. Epub 2021 Mar 17.
Systemic treatment of rheumatoid arthritis has been accompanied with several side effects. This study attempts to reduce leflunomide systemic side effects besides increasing its joint healing outcomes via formulation of layer-by-layer coated, leflunomide-loaded solid lipid nanoparticles (SLNs). SLNs were coated with chitosan (CS) followed by folic acid (FA). FA-CS-SLNs were about 284.9 nm and carried negative surface charge. FA-CS-SLNs showed sustained release profile for 168 h. Results of oral administration of FA-CS-SLNs in rats with adjuvant-induced arthritis revealed improved joint healing and reduced hepatotoxicity compared with leflunomide suspension. This may be attributed to the ability of FA-CS-SLNs to actively target FA receptors that are overexpressed in inflamed rheumatic joints in addition to innate joint healing properties of CS.
类风湿关节炎的系统治疗伴随着一些副作用。本研究试图通过层状包衣、负载来氟米特的固体脂质纳米粒(SLNs)来减少来氟米特的全身副作用,同时提高其关节愈合效果。SLNs 用壳聚糖(CS)包衣,然后用叶酸(FA)包衣。FA-CS-SLNs 的粒径约为 284.9nm,带负表面电荷。FA-CS-SLNs 表现出 168 小时的持续释放。与来氟米特混悬液相比,在佐剂诱导关节炎大鼠中口服给予 FA-CS-SLNs 可改善关节愈合并降低肝毒性。这可能归因于 FA-CS-SLNs 能够主动靶向在炎症性风湿关节中过度表达的 FA 受体,以及 CS 的固有关节愈合特性。