Details

Autor(en) / Beteiligte

• Galdopórpora, Juan M
• Martinena, Camila
• Bernabeu, Ezequiel
• Riedel, Jennifer
• Palmas, Lucia
• Castangia, Ines
• Manca, Maria Letizia
• Garcés, Mariana
• Lázaro-Martinez, Juan
• Salgueiro, Maria Jimena
• Evelson, Pablo
• Tateosian, Nancy Liliana
• Chiappetta, Diego Andres
• Moretton, Marcela Analia

Titel

Inhalable Mannosylated Rifampicin-Curcumin Co-Loaded Nanomicelles with Enhanced In Vitro Antimicrobial Efficacy for an Optimized Pulmonary Tuberculosis Therapy

Ist Teil von

• Pharmaceutics, 2022-04, Vol.14 (5), p.959

Ort / Verlag

Switzerland: MDPI AG

Erscheinungsjahr

2022

Quelle

EZB Electronic Journals Library

Beschreibungen/Notizen

• Among respiratory infections, tuberculosis was the second deadliest infectious disease in 2020 behind COVID-19. Inhalable nanocarriers offer the possibility of actively targeting anti-tuberculosis drugs to the lungs, especially to alveolar macrophages (cellular reservoirs of the ). Our strategy was based on the development of a mannose-decorated micellar nanoformulation based in Soluplus to co-encapsulate rifampicin and curcumin. The former is one of the most effective anti-tuberculosis first-line drugs, while curcumin has demonstrated potential anti-mycobacterial properties. Mannose-coated rifampicin (10 mg/mL)-curcumin (5 mg/mL)-loaded polymeric micelles (10% / ) demonstrated excellent colloidal properties with micellar size ~108 ± 1 nm after freeze-drying, and they remain stable under dilution in simulated interstitial lung fluid. Drug-loaded polymeric micelles were suitable for drug delivery to the deep lung with lung accumulation, according to the in vitro nebulization studies and the in vivo biodistribution assays of radiolabeled (99mTc) polymeric micelles, respectively. Hence, the nanoformulation did not exhibit hemolytic potential. Interestingly, the addition of mannose significantly improved (5.2-fold) the microbicidal efficacy against H37Rv of the drug-co-loaded systems in comparison with their counterpart mannose-free polymeric micelles. Thus, this novel inhaled nanoformulation has demonstrated its potential for active drug delivery in pulmonary tuberculosis therapy.