Introduction

The Chemokine Receptor 2 (CCR2), is a pro-inflammatory action molecule and widely expressed in our body. Several studies conducted on CCR2 suggested that its transient inhibition (as opposed to a sustained inhibition) gave better structural results in mouse models affected by osteoarthritis (OA), providing important considerations in the role of inflammation in its pathogenesis: Inflammation plays a key role in healing after an injury, but when inflammation is not limited and becomes chronic, it can perpetuate and amplify the destruction and remodeling of joints. Therefore, it became necessary a system that modules CCR2, fundamental in limiting inflammation and therefore in the treatment of OA.

Technical features

The object of the invention is a composition comprising one or more prism-shaped microparticles with three or more sides, with a height and length of each side between 5 and 50 pm, comprising at least one polymer and at least one CCR2 inhibitor. The particles are injected locally: it was discovered in fact, that such microparticles when injected directly into the joint provide a prolonged release of the therapeutic agents loaded for several weeks after a single injection, increasing the therapeutic efficacy. This together with the unique mechanical characteristics of the particles allows to create an intrarticular deposit that promotes the continuous inhibition of the CCR2 receptor in the articulation of a subject with OA. The localized release of the drug allows to avoid systemic inhibition of CCR2, which is accompanied by the numerical reduction of the anti-inflammatory regulatory T cells, thereby worsening inflammation, advancing OA and hindering the beneficial action observed in the cartilage and bone compartment. TRL 4/5.

Possible Applications

• Treatment of osteoarthritis and/or other chronic pathologies that currently require daily drugs administration.

Advantages

• Local administration, avoiding side effects associated with the systemic and daily administration of the CCR2 inhibitor
• Improved efficacy on cartilage and bone structure, both in the early and late stages of OA, combining pharmacological and mechanical effects
• Better solubility than a single CCR2 inhibitor
• Possibility of modulating the release profile of the drug, changing some characteristics of microparticles, such as the height and amount of polymer used