Biological assessment of self-assembled polymeric micelles for pulmonary administration of insulin.
UNLABELLED
Pulmonary delivery of drugs for both local and systemic action has gained new attention over the last decades. In this work, different amphiphilic polymers (Soluplus®, Pluronic® F68, Pluronic® F108 and Pluronic® F127) were used to produce lyophilized formulations for inhalation of insulin. Development of stimuli-responsive, namely glucose-sensitive, formulations was also attempted with the addition of phenylboronic acid (PBA). Despite influencing the in vitro release of insulin from micelles, PBA did not confer glucose-sensitive properties to formulations. Lyophilized powders with aerodynamic diameter (<6 μm) compatible with good deposition in the lungs did not present significant in vitro toxicity for respiratory cell lines. Additionally, some formulations, in particular Pluronic® F127-based formulations, enhanced the permeation of insulin through pulmonary epithelial models and underwent minimal internalization by macrophages in vitro. Overall, formulations based on polymeric micelles presenting promising characteristics were developed for the delivery of insulin by inhalation.


FROM THE CLINICAL EDITOR
The ability to deliver other systemic drugs via inhalation has received renewed interests in the clinical setting. This is especially true for drugs which usually require injections for delivery, like insulin. In this article, the authors investigated their previously developed amphiphilic polymers for inhalation of insulin in an in vitro model. The results should provide basis for future in vivo studies.
['Andrade|Fernanda|F|', 'das Neves|José|J|', 'Gener|Petra|P|', 'Schwartz|Simó|S|', 'Ferreira|Domingos|D|', 'Oliva|Mireia|M|', 'Sarmento|Bruno|B|']
D000280:Administration, Inhalation D001897:Boronic Acids D018929:Cell Culture Techniques D002626:Chemistry, Pharmaceutical D016503:Drug Delivery Systems D005947:Glucose D006801:Humans D007328:Insulin D008823:Micelles D010539:Permeability D010587:Phagocytosis D011108:Polymers
Polymeric micelles Inhalation Cytotoxicity Permeability Phagocytosis Protein delivery