Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles.

Autor:	Madrid Sani AT; Bionanomanufacturing Center, Technological Research Institute, São Paulo, Brazil.; Department of Biochemical and Pharmaceutical Technology, University of São Paulo, São Paulo, Brazil., Ramos-Rocha KLV; Bionanomanufacturing Center, Technological Research Institute, São Paulo, Brazil.; Department of Biochemical and Pharmaceutical Technology, University of São Paulo, São Paulo, Brazil., Sarcinelli MA; Laboratory of Micro and Nanotechnology, Fundação Oswaldo Cruz, Rio de Janeiro, Brazil., Chaves MHDC; Laboratory of Micro and Nanotechnology, Fundação Oswaldo Cruz, Rio de Janeiro, Brazil., Rocha HVA; Laboratory of Micro and Nanotechnology, Fundação Oswaldo Cruz, Rio de Janeiro, Brazil., Léo P; Bionanomanufacturing Center, Technological Research Institute, São Paulo, Brazil., Cerize NNP; Bionanomanufacturing Center, Technological Research Institute, São Paulo, Brazil., Zanin MHA; Bionanomanufacturing Center, Technological Research Institute, São Paulo, Brazil., Feitosa VA; Department of Biochemical and Pharmaceutical Technology, University of São Paulo, São Paulo, Brazil., Rangel-Yagui CO; Department of Biochemical and Pharmaceutical Technology, University of São Paulo, São Paulo, Brazil.
Jazyk:	angličtina
Zdroj:	Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques [J Pharm Pharm Sci] 2024 Oct 14; Vol. 27, pp. 13635. Date of Electronic Publication: 2024 Oct 14 (Print Publication: 2024).
DOI:	10.3389/jpps.2024.13635
Abstrakt:	The COVID-19 pandemic has raised concern regarding respiratory system diseases and oral inhalation stands out as an attractive non-invasive route of administration for pulmonary diseases such as chronic bronchitis, cystic fibrosis, COVID-19 and community-acquired pneumonia. In this context, we encapsulated azithromycin in polycaprolactone nanoparticles functionalized with phospholipids rich in dipalmitoylphosphatidylcholine and further produced a fine powder formulation by spray drying with monohydrated lactose. Nanoparticles obtained by the emulsion/solvent diffusion-evaporation technique exhibited a mean hydrodynamic diameter around 195-228 nm with a narrow monomodal size distribution (PdI < 0.2). Nanoparticle dispersions were spray-dried at different inlet temperatures, atomizing air-flow, aspirator air flow, and feed rate, using lactose as a drying aid, resulting in a maximal process yield of 63% and an encapsulation efficiency of 83%. Excipients and the dry powder formulations were characterized in terms of morphology, chemical structure, thermal analyses and particle size by SEM, FTIR, DSC/TGA and laser light diffraction. The results indicated spherical particles with 90% at 4.06 µm or below, an adequate size for pulmonary delivery. Aerosolization performance in a NGI confirmed good aerodynamic properties. Microbiological assays showed that the formulation preserves AZM antimicrobial effect against Staphylococcus aureus and Streptococcus pneumoniae strains, with halos above 18 mm. In addition, no formulation-related cytotoxicity was observed against the human cell lines BEAS-2B (lung epithelial), HUVEC (endothelial) and HFF1 (fibroblasts). Overall, the approach described here allows the production of AZM-PCL nanoparticles incorporated into inhalable microparticles, enabling more efficient pulmonary therapy of lung infections. Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. (Copyright © 2024 Madrid Sani, Ramos-Rocha, Sarcinelli, Chaves, Rocha, Léo, Cerize, Zanin, Feitosa and Rangel-Yagui.)
Databáze:	MEDLINE
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