Optimization of the bioavailability of CXCR1/CXCR2 receptor antagonists using nanoformulations

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CXCL cytokines, in particular interleukin 8/CXCL, regulate the processes of angiogenesis and inflammation that are common to a number of pathologies such as cardiovascular disease, cancer, diabetic retinopathy and age-related macular degeneration. The CXCL cytokines comprise two subclasses, ELR-CXCL, which are anti-angiogenic and anti-inflammatory, and ELR+CXCL, which are pro-angiogenic and pro-inflammatory and act via the intermediate receptors CXCR1 and CXCR2. Competitive antagonists of these cellular IL-8 receptors, with their ability to counter inflammation and neo-angiogenesis, offer prospects for the treatment of various pathologies combining these two processes. Nevertheless, the solubility characteristics of these molecules limit their bioavailability and require optimization, through the synthesis of more hydrophilic analogues and/or the development of optimized galenic formulations.

In collaboration with Pr Luc Demange and Dr Diana Lamaa (CiTCoM UMR CNRS 8038), who are synthesizing new CXCR1/CXCR2 receptor antagonists, UTCBS is developing nanoemulsion-type formulations, in particular for the topical treatment of age-related macular degeneration, as part of Dr Mitta Pierre’s university thesis.

This project is under the responsibility of Pr Christine CHARRUEAU.

See the presentation of the thesis of Mitta Pierre

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