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Remdesivir-loaded bis-MPA hyperbranched dendritic nanocarriers for pulmonary delivery.
Halevas, Eleftherios; Mavroidi, Barbara; Kokotidou, Chrysoula; Moschona, Alexandra; Sagnou, Marina; Mitraki, Anna; Litsardakis, George; Pelecanou, Maria.
  • Halevas E; Institute of Biosciences & Applications, National Centre for Scientific Research "Demokritos", 15310, Athens, Greece.
  • Mavroidi B; Institute of Biosciences & Applications, National Centre for Scientific Research "Demokritos", 15310, Athens, Greece.
  • Kokotidou C; Department of Materials Science and Technology University of Crete, Heraklion, 70013, Crete, Greece.
  • Moschona A; Institute for Electronic Structure and Laser FORTH N. Plastira 100, Heraklion, 70013, Crete, Greece.
  • Sagnou M; Laboratory of Organic Chemistry, Department of Chemical Engineering, Aristotle University of Thessaloniki, Thessaloniki, 54124, Greece.
  • Mitraki A; Laboratory of Natural Resources and Renewable Energies, Chemical Process and Energy Resources Institute, Centre for Research and Technology-Hellas (CERTH), Thessaloniki, 57001, Greece.
  • Litsardakis G; Institute of Biosciences & Applications, National Centre for Scientific Research "Demokritos", 15310, Athens, Greece.
  • Pelecanou M; Department of Materials Science and Technology University of Crete, Heraklion, 70013, Crete, Greece.
J Drug Deliv Sci Technol ; 75: 103625, 2022 Sep.
Article in English | MEDLINE | ID: covidwho-1977460
ABSTRACT
Remdesivir is the only clinically available antiviral drug for the treatment of COVID-19. However, its very limited aqueous solubility confines its therapeutic activity and the development of novel inhaled nano-based drug delivery systems of remdesivir for enhanced lung tissue targeting and efficacy is internationally pursued. In this work 2,2-bis(hydroxymethyl)propionic acid (bis-MPA) hyperbranched dendritic nano-scaffolds were employed as nanocarriers of remdesivir. The produced nano-formulations, empty and loaded, consisted of monodisperse nanoparticles with spherical morphology and neutral surface charge and sizes ranging between 80 and 230 nm. The entrapment efficiency and loading capacity of the loaded samples were 82.0% and 14.1%, respectively, whereas the release of the encapsulated drug was complete after 48 h. The toxicity assays in healthy MRC-5 lung diploid fibroblasts and NR8383 alveolar macrophages indicated their suitability as potential remdesivir carriers in the respiratory system. The novel nano-formulations are non-toxic in both tested cell lines, with IC50 values higher than 400 µΜ after 72 h treatment. Moreover, both free and encapsulated remdesivir exhibited very similar IC50 values, at the range of 80-90 µM, while its aqueous solubility was increased, overall presenting a suitable profile for application in inhaled delivery of therapeutics.
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Full text: Available Collection: International databases Database: MEDLINE Type of study: Prognostic study Language: English Journal: J Drug Deliv Sci Technol Year: 2022 Document Type: Article Affiliation country: J.jddst.2022.103625

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Full text: Available Collection: International databases Database: MEDLINE Type of study: Prognostic study Language: English Journal: J Drug Deliv Sci Technol Year: 2022 Document Type: Article Affiliation country: J.jddst.2022.103625