Liposomal formulation for the treatment of fibrogenic lung disorders

Our liposome formulation is decorated with hyaluronic acid (HA) at a specific molecular weight range. This allows the interaction of HA liposomes with CD44, the natural receptor of HA that is highly expressed by primary myofibroblasts from lung of affected patients and by inflammatory cells. It is important to note that CD44 is not expressed by normal non activated epithelial cells, so we are able to spare bronchiolar and alveolar epithelium thus avoiding toxicity at this level and promoting repair of injured tissue. By means of this approach we gained interesting and significant results both in vitro (on primary cells obtained by patients with pulmonary fibrosis or bronchiolitis obliterans syndrome) and in vivo (specific animal models of disease) encapsulating a tyrosine-kinase inhibitor. The administration of drugs directly into the lungs offers the great advantage of limiting systemic toxicity and obtaining high drug concentrations in the target tissue. In addition, this approach, can preferentially direct drugs to specific disease effectors.

The delivery of drugs through aerosol administration of liposomes is an excellent solution for several reasons:

• they are biocompatible and biodegradable
• they increase the presence of drug in the deep lung reducing systemic absorption
• they allow the release of the drug over time and in a controlled manner
• they target fibrogenic cells of interest

Filing date: 24/08/2021

Application number: 102021000022253