Amelioration of murine experimental colitis using biocompatible cyclosporine A lipid carriers.
Fiche publication
Date publication
juin 2021
Journal
Drug delivery and translational research
Auteurs
Membres identifiés du Cancéropôle Est :
Pr BEDUNEAU Arnaud
Tous les auteurs :
Scarcello E, Abdel-Mottaleb MMA, Beduneau A, Moulari B, Pellequer Y
Lien Pubmed
Résumé
Lipoproteins are biodegradable and biocompatible natural carriers that can be utilized for the transport of hydrophobic drugs, such as cyclosporin A (CycloA), a calcineurin inhibitor utilized for the inflammatory bowel disease, such as ulcerative colitis. A major limitation in the drug treatment of inflammatory bowel disease is the inability to deliver the drug selectively toward the inflamed tissues. Nanotechnology-based drug delivery systems have led to an amelioration of the therapeutic selectivity, but still the majority of the entrapped drug is eliminated without exercising a therapeutic effect. The present study aimed to prepare three lipoprotein formulations (HDL-, LDL-, and VLDL-based) loaded with cyclosporin A for the treatment of colitis in a murine model. After an intravenous injection of a drug dose of 2 mg/kg, clinical activity (colon weight/length ratio) and therapeutic effects (evaluated by the inflammatory markers MPO and TNF-α) were compared with those of the untreated colitis control group. All CycloA-containing lipoproteins reduced clinical activity, with a significant decrease in the case of LDL-CycloA formulation, which also led to the higher therapeutic effect.
Mots clés
Cyclosporin A, LDL, Lipoproteins, TNBS murine model, Ulcerative colitis
Référence
Drug Deliv Transl Res. 2021 06;11(3):1301-1308