Paulo R. Lino1, Cláudia Costa1, Nichal Gentilal1, Maria I. Lopes1, Andreia Dias1,2, Mykaella Mestre1,3, Beatriz Gamelas1,3, André Ribeiro1, Joana Diogo1, Patrícia Henriques1, Filipa Ferreira1, Rui Churro1, Susana I. Saldanha1, Marco Galésio1 & Alexandre J.S. Ribeiro1
1Hovione FarmaCiência SA, Lumiar, 1649-038, Portugal
2Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, 1749-016, Portugal.
3Institute for Bioengineering and Biosciences (iBB), Lisboa, 1049-001, Portugal
Summary
This study investigates the potential of Dispersome®, a novel excipient platform using the protein β-lactoglobulin (BLG), for applications in dry powder formulations intended for respiratory drug delivery (pulmonary and nasal). BLG was used as an excipient to produce dispersible, high-density composite particles via spray drying. Key outcomes of the study include: (i) optimization of spray drying parameters to yield BLG particles with fine particle fractions reaching up to 90%; (ii) demonstrated physicochemical compatibility of BLG with active pharmaceutical ingredients (API) such as fluticasone furoate (FF) and Tobramycin (TOB); (iii) successful stabilization of amorphous dispersions containing up to 75% (w/w) drug load of FF and TOB; (iv) efficient nasal deposition of BLG-based formulations; and (v) evidence of pulmonary and systemic clearance within 24 hours post-inhalation in rats with no significant immune response. These findings support the further development of BLG as an excipient for respiratory drug delivery.
Key Message