10.1007/s40097-022-00476-3

Polymeric nanoparticles and nanomicelles of hydroxychloroquine co-loaded with azithromycin potentiate anti-SARS-CoV-2 effect

  • Aline Oliveira da Siliva de Barros1,
  • Suyene Rocha Pinto1,
  • Sara Rhaissa Rezende dos Reis1,
  • Eduardo Ricci-Junior2,
  • Luciana Magalhães Rebelo Alencar3,
  • Nancy Cristina Junqueira Bellei4,
  • Luiz Ramos Mário Janini5,
  • Juliana Terzi Maricato5,
  • Daniela Santoro Rosa5,
  • Ralph Santos-Oliveira*6,
  1. Laboratory of Nanoradiopharmacy and Synthesis of New Radiopharmaceuticals, Nuclear Engineering Institute, Brazilian Nuclear Energy Commission, Rio de Janeiro, BR
  2. Galenical Development Laboratory, College of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, BR
  3. Department of Physics, Federal University of Maranhão, Maranhão, BR
  4. Department of Medicine, Federal University of São Paulo, São Paulo, BR
  5. Department of Microbiology, Immunology and Parasitology, Federal University of São Paulo, São Paulo, BR
  6. Laboratory of Nanoradiopharmacy and Synthesis of New Radiopharmaceuticals, Nuclear Engineering Institute, Brazilian Nuclear Energy Commission, Rio de Janeiro, BR Laboratory of Radiopharmacy and Nanoradiopharmaceuticals, Zona Oeste State University, Rio de Janeiro, BR

Published in Issue 26-02-2022

How to Cite

de Barros, A. O. da S., Pinto, S. R., dos Reis, S. R. R., Ricci-Junior, E., Alencar, L. M. R., Bellei, N. C. J., Janini, L. R. M., Maricato, J. T., Rosa, D. S., & Santos-Oliveira, R. (2022). Polymeric nanoparticles and nanomicelles of hydroxychloroquine co-loaded with azithromycin potentiate anti-SARS-CoV-2 effect. Journal of Nanostructure in Chemistry, 13(2 (April 2023). https://doi.org/10.1007/s40097-022-00476-3
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Abstract

Abstract The outbreak of coronavirus (COVID-19) has put the world in an unprecedented scenario. To reestablish the world routine as promote the effective treatment of this disease, the world is looking for new (and old) drug that can efficiently kill the virus. In this study, we have developed two nanosystems: polymeric nanoparticles and nanomicelles-based on hydroxychloroquine and azithromycin. The nanosystem was fully characterized by AFM and DLS techniques. Also, the nanosystems were radiolabeled with 99m Tc and pulmonary applied (installation) in vivo to evaluate the biological behavior. The toxicity of both nanosystem were evaluated in primary cells (FGH). Finally, both nanosystems were evaluated in vitro against the SARS-CoV-2. The results demonstrated that the methodology used to produce the nanomicelles and the nanoparticle was efficient, the characterization showed a nanoparticle with a spherical shape and a medium size of 390 nm and a nanomicelle also with a spherical shape and a medium size of 602 nm. The nanomicelles were more efficient (~ 70%) against SARS-CoV-2 than the nanoparticles. The radiolabeling process with 99m Tc was efficient (> 95%) in both nanosystems and the pulmonary application demonstrated to be a viable route for both nanosystems with a local retention time of approximately, 24 h. None of the nanosystems showed cytotoxic effect on FGH cells, even in high doses, corroborating the safety of both nanosystems. Thus, claiming the benefits of the nanotechnology, especially with regard the reduced adverse we believe that the use of nanosystems for COVID-19 treatment can be an optimized choice. Graphical abstract

Keywords

  • Drug,
  • Nanotechnology,
  • COVID-19,
  • SARS-CoV-2,
  • Virus,
  • Treatment

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