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Development of a Carrier-Free Dry Powder Ofloxacin Formulation With Enhanced Aerosolization Properties.
Metadata
Journaljournal of pharmaceutical sciences2.997Date
2020 Jun 04
4 months ago
Type
Journal Article
Volume
2020-Sep / 109 : 2787-2797
Author
Ceschan NE 1, Rosas MD 2, Olivera ME 3, Dugour AV 4, Figueroa JM 4, Bucalá V 5, Ramírez-Rigo MV 2
Affiliation
  • 2. Planta Piloto de Ingeniería Química (PLAPIQUI), Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET) - Universidad Nacional del Sur (UNS), Camino La Carrindanga km 7, 8000 Bahía Blanca, Argentina; Departamento de Biología, Bioquímica y Farmacia, UNS, San Juan 670, 8000 Bahía Blanca, Argentina.
  • 3. Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina; Unidad de Tecnología Farmacéutica (UNITEFA-CONICET), Córdoba, Argentina.
  • 4. Centro de Biología Respiratoria (CEBIR), Fundación Pablo Cassará, Saladillo 2452, C1440FFX Ciudad Autónoma de Buenos Aires, Argentina.
  • 5. Planta Piloto de Ingeniería Química (PLAPIQUI), Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET) - Universidad Nacional del Sur (UNS), Camino La Carrindanga km 7, 8000 Bahía Blanca, Argentina; Departamento de Ingeniería Química, UNS, Avenida Alem 1253, 8000 Bahía Blanca, Argentina.
Doi
PMIDMESH
Abstract
Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibiotic activity against the bacteria that causes TB (M. tuberculosis). In this work, ionic complexes, composed by hyaluronic acid (HA) and OF, with different neutralization degrees, were prepared and processed by spray drying (SD) to obtain powders for inhalatory administration. Combining a formulation with high neutralization degree, high SD atomization air flowrate and the use of a high-performance collection cyclone, very good process yields were obtained. Carrier-free formulations with a loading of 0.39-0.46 gOF/gpowder showed excellent emitted, fine particle, and respirable fractions for capsule loadings of 25 and 100 mg. The ionic complexes demonstrated higher mucoadhesion than pure OF and HA. The best formulation did not affect CALU-3 cell viability up to a dose 6.5 times higher than the MIC90 reported to treat multi-drug resistant TB.
Keywords: Cell viability Drug-excipient interaction Fluoroquinolones Hyaluronic acid Inhalation Mucoadhesive Multi-drug resistant tuberculosis Spray drying
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J Pharm Scijournal of pharmaceutical sciences
Metadata
LocationUnited States
FromELSEVIER SCIENCE INC

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