Topically applied phospho-sulindac hydrogel is efficacious and safe in the treatment of experimental arthritis in rats.
Topically applied phospho-sulindac hydrogel is efficacious and safe in the treatment of experimental arthritis in rats.
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局部施用的磷酸硫酸盐水凝胶在治疗大鼠实验性关节炎方面是有效且安全的。
DOI：
10.1007/s11095-012-0953-8
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发表时间：
2013-06
影响因子：
3.7
通讯作者：
Rigas, Basil
中科院分区：
文献类型：
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作者：
Mattheolabakis, George;Mackenzie, Gerardo G.;Huang, Liqun;Ouyang, Nengtai;Cheng, Ka Wing;Rigas, Basil
Formulate phospho-sulindac (P-S, OXT-328) in a Pluronic hydrogel to be used as a topical anti-inflammatory agent and study its efficacy, safety and pharmacokinetics in an arthritis model. LEW/crlBR rats with Freund's adjuvant-induced arthritis were treated with P-S formulated in Pluronic hydrogel (PSH). We determined the clinical manifestations of arthritis including the locomotor activity of the rats; evaluated joints for inflammation, bone resorption, cartilage damage, COX-2 expression and NF-κB activation; assayed plasma IL-6 and IL-10 levels; and studied the pharmacokinetics of P-S in rats after topical or oral administration. PSH applied at the onset of arthritis or when arthritis was fully developed, suppressed it by 56–82%, improved the locomotor activity of the rats 2.1–4.4 fold, suppressed synovial inflammation, bone resorption, cartilage damage, NF-κB activation and COX-2 expression but not plasma IL-6 and IL-10 levels. There were no side effects. PSH produced rapidly high local levels of P-S with < 14% of P-S reaching the circulation, while orally administered PS was rapidly metabolized generating much lower joint levels of P-S. Topical application of PSH is efficacious and safe in the treatment of Freund's adjuvant-induced arthritis; has a favorable pharmacokinetic profile; and likely acts by suppressing key pro-inflammatory signaling pathways.
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影响因子：
15.9
作者：
Anderson, GD;Hauser, SD;Gregory, SA
通讯作者：
Gregory, SA
影响因子：
5.8
作者：
Mattheolabakis, George;Lagoumintzis, George;Avgoustakis, Konstantinos
通讯作者：
Avgoustakis, Konstantinos
影响因子：
2.8
作者：
Farkouh, Michael E.;Greenberg, Bruce P.
通讯作者：
Greenberg, Bruce P.
影响因子：
3.9
作者：
Foster, Beth;Cosgrove, Terence;Hammouda, Boualem
通讯作者：
Hammouda, Boualem
DOI：
10.1002/art.20924
发表时间：
2005-02-15
期刊：
ARTHRITIS & RHEUMATISM-ARTHRITIS CARE & RESEARCH
影响因子：
--
作者：
Eurenius, E;Stenström, CH
通讯作者：
Stenström, CH