Dexamethasone palmitate (Synonyms: Dexamethasone 21-palmitate, DXP, Limethason)

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.