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Dexamethasone palmitate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dexamethasone palmitate图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
地塞米松棕榈酸酯 (DXP) 是地塞米松的前药。

Cell lines

RAW 264.7 cells

Preparation Method

After 24 h of incubation with 100 μg/mL Dexamethasone palmitate, cell supernatants were collected and frozen at 20 C until analysis was performed. Cells were detached and counted.

Reaction Conditions

100 μg/mL Dexamethasone palmitate,24h

Applications

A decrease of cytokines concentration was clearly observed resulting from the anti-inflammatory effect of Dexamethasone palmitate-NPs.

Animal models

Brown Norway male rats

Preparation Method

Choroidal neovascularization (CNV) was induced with a 532-nm argon laser photocoagulator in the right eyes of the anesthetized animals. Following the laser procedure on day 0 supratemporal IVT injections of either the vehicle [phosphate- buffered saline (PBS); 0.8% Dexamethasone palmitate emulsion (4 μg Dexamethasone palmitate; 0.5 μL), and Kenacort were administered to the treated right eyes.

Dosage form

4 μg Dexamethasone palmitate;0.5 μL

Applications

Rat efficacy data demonstrated that IVT administration of Dexamethasone palmitate emulsions is effective for delivering therapeutic concentrations of DXM at the level of the choroid.

产品描述

Dexamethasone palmitate (DXP), a lipophilic prodrug of Dexamethasone (DXM), is a glucocorticoid receptor agonist with a 47-fold lower affinity for the glucocorticoid receptor than DXM[1].

A decrease of cytokines concentration was clearly observed resulting from the anti-inflammatory effect of Dexamethasone palmitate-NPs .the MCP-1 chemokine was strongly and significantly reduced by Dexamethasone palmitate-NPs and TNFα in presence of LPS[2].

Rat efficacy data demonstrated that IVT administration of Dexamethasone palmitate emulsions is effective for delivering therapeutic concentrations of DXM at the level of the choroid[2]. Dexamethasone palmitate-NPs could benefit from the typical high vascular permeability of inflamed joints and diffuse passively to accumulate and be retained in the diseased sites. This accumulation in inflamed joints led to improvement of the joint inflammation and eventually disease remission[3].

References:
[1]:Romero IA, Radewicz K, Jubin E, Michel CC, Greenwood J, Couraud PO, Adamson P. Changes in cytoskeletal and tight junctional proteins correlate with decreased permeability induced by dexamethasone in cultured rat brain endothelial cells. Neurosci Lett. 2003 Jun 26;344(2):112-6. doi: 10.1016/s0304-3940(03)00348-3. PMID: 12782340.
[2]: Daull P, Paterson CA, Kuppermann BD, Garrigue JS. A preliminary evaluation of dexamethasone palmitate emulsion: a novel intravitreal sustained delivery of corticosteroid for treatment of macular edema. J Ocul Pharmacol Ther. 2013 Mar;29(2):258-69. doi: 10.1089/jop.2012.0044. Epub 2013 Jan 18. PMID: 23331052.
[3]: Lorscheider M, Tsapis N, Ur-Rehman M, Gaudin F, Stolfa I, Abreu S, Mura S, Chaminade P, Espeli M, Fattal E. Dexamethasone palmitate nanoparticles: An efficient treatment for rheumatoid arthritis. J Control Release. 2019 Feb 28;296:179-189. doi: 10.1016/j.jconrel.2019.01.015. Epub 2019 Jan 16. PMID: 30659904.