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Eur J Pharm Biopharm ; 130: 30-38, 2018 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29890256

RESUMEN

In this paper, we shed light on the potential of Pluronic® mixed micelles in lung delivery of poorly water-soluble drugs. To this purpose, Pluronic® P123/F127 mixed micelles (PMM), exhibiting superior stability in biological fluids, were loaded with budesonide (BUD), a model hydrophobic corticosteroid, and fully investigated focusing on their stability in pulmonary-relevant media, transport through the mucus barrier and aerodynamic behaviour in vitro. Then, lung bio-distribution and efficacy were evaluated in vivo, after intra-tracheal administration in rats. PMM showed excellent stability in saline, mucin, artificial airway mucus and simulated interstitial lung fluid. Likely due to their small size coupled with the hydrophilic biofouling shell, PMM did not interact with mucin and consequently diffused through artificial mucus. BUD was loaded with high efficiency in PMM and released at sustained rate in artificial mucus. BUD-PMM dispersion in saline was efficiently delivered through a common jet nebulizer without aggregation. After intratracheal administration in rats, PMM labelled with Rhodamine B persisted in the lung up to 24 h, while serum levels rapidly dropped. Finally, the effects of BUD-PMM in a rat model of lung inflammation induced by intra-tracheal aerosolization of lipopolysaccharide (LPS) from E. coli were investigated. Of note, a single intra-tracheal aerosolization of BUD-PMM significantly reduced bronchoalveolar neutrophil infiltration and the expression of protein/enzymes derived from the arachidonic acid cascade induced by LPS, whereas a control BUD aqueous suspension showed a weaker effect. Overall, this study demonstrates that inhalable formulations of PMM can be considered as a platform for local delivery of hydrophobic drugs at lungs worth of further consideration.


Asunto(s)
Budesonida/administración & dosificación , Sistemas de Liberación de Medicamentos , Pulmón/metabolismo , Poloxámero/química , Administración por Inhalación , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/química , Antiinflamatorios/farmacocinética , Budesonida/química , Budesonida/farmacocinética , Modelos Animales de Enfermedad , Portadores de Fármacos/química , Interacciones Hidrofóbicas e Hidrofílicas , Lipopolisacáridos/toxicidad , Masculino , Micelas , Nebulizadores y Vaporizadores , Tamaño de la Partícula , Neumonía/tratamiento farmacológico , Ratas , Ratas Wistar , Factores de Tiempo , Distribución Tisular
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