Amelioration of murine experimental colitis using biocompatible cyclosporine A lipid carriers
Scarcello, Eleonora; Abdel-Mottaleb, Mona; Beduneau, Arnaud; Moulari, Brice; Pellequer, Yann;
Abstract
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. [Figure not available: see fulltext.]
Other data
Title | Amelioration of murine experimental colitis using biocompatible cyclosporine A lipid carriers | Authors | Scarcello, Eleonora; Abdel-Mottaleb, Mona ; Beduneau, Arnaud; Moulari, Brice; Pellequer, Yann | Keywords | Cyclosporin A;LDL;Lipoproteins;TNBS murine model;Ulcerative colitis | Issue Date | 1-Jun-2021 | Publisher | SPRINGER HEIDELBERG | Journal | Drug Delivery and Translational Research | Volume | 11 | Start page | 1301 | End page | 1308 | ISSN | 2190393X | DOI | 10.1007/s13346-020-00835-z | PubMed ID | 32794147 | Scopus ID | 2-s2.0-85089375029 | Web of science ID | WOS:000559427500002 |
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