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A ready-to-use dry powder formulation based on protamine nanocarriers for pulmonary drug delivery

Authors :
Sandra Robla
Rubén Varela Calviño
Rita Ambrus
Noemi Csaba
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Bioquímica e Bioloxía Molecular
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Source :
European Journal of Pharmaceutical Sciences. 185:106442
Publication Year :
2023
Publisher :
Elsevier BV, 2023.

Abstract

The use of oral antibiotic therapy for the treatment of respiratory diseases as tuberculosis has promoted the appearance of side effects as well as resistance to these treatments. The low solubility, high metabolism, and degradation of drugs as rifabutin, have led to the use of combined and prolonged therapies, which difficult patient compliance. In this work, we develop inhalable formulations from biomaterials such as protamine to improve the therapeutic effect. Rifabutin-loaded protamine nanocapsules (NCs) were prepared by solvent displacement method and were physico-chemically characterized and evaluated for their dissolution, permeability, stability, cytotoxicity, hemocompatibility, internalization, and aerodynamic characteristics after a spray-drying procedure. Protamine NCs presented a size of around 200 nm, positive surface charge, and drug association up to 54%. They were stable as suspension under storage, as well as in biological media and as a dry powder after lyophilization in the presence of mannitol. Nanocapsules showed a good safety profile and cellular uptake with no tolerogenic effect on macrophages and showed good compatibility with red blood cells. Moreover, the aerodynamic evaluation showed a fine particle fraction deposition up to 30% and a mass median aerodynamic diameter of about 5 µm, suitable for the pulmonary delivery of therapeutics This research was funded by Ministerio de Ciencia e Innovacion RETOS - PID2019-107500RB-I00, Ministry of Human Capacities, Hungary grant TKP2021-EGA-32 and the Erasmus+ program of the European Union SI

Details

ISSN :
09280987
Volume :
185
Database :
OpenAIRE
Journal :
European Journal of Pharmaceutical Sciences
Accession number :
edsair.doi.dedup.....7a35c254ba9244e5a7907b16c49ad8cb
Full Text :
https://doi.org/10.1016/j.ejps.2023.106442