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Spray-dried lactose-leucine microparticles for pulmonary delivery of antimycobacterial nanopharmaceuticals

Thiyagarajan, D.; Huck, B.; Nothdurft, B.; Koch, M.; Rudolph, D. 1; Rutschmann, M. 1; Feldmann, C. 1; Hozsa, C.; Furch, M.; Besecke, K. F. W.; Gieseler, R. K.; Loretz, B.; Lehr, C.-M.
1 Institut für Anorganische Chemie (AOC), Karlsruher Institut für Technologie (KIT)


Pulmonary delivery of nanocarriers for novel antimycobacterial compounds is challenging because the aerodynamic properties of nanomaterials are sub-optimal for such purposes. Here, we report the development of dry powder formulations for nanocarriers containing benzothiazinone 043 (BTZ) or levofloxacin (LVX), respectively. The intricacy is to generate dry powder aerosols with adequate aerodynamic properties while maintaining both nanostructural integrity and compound activity until reaching the deeper lung compartments. Microparticles (MPs) were prepared using vibrating mesh spray drying with lactose and leucine as approved excipients for oral inhalation drug products. MP morphologies and sizes were measured using various biophysical techniques including determination of geometric and aerodynamic mean sizes, X-ray diffraction, and confocal and focused ion beam scanning electron microscopy. Differences in the nanocarriers’ characteristics influenced the MPs’ sizes and shapes, their aerodynamic properties, and, hence, also the fraction available for lung deposition. Spay-dried powders of a BTZ nanosuspension, BTZ-loaded silica nanoparticles (NPs), and LVX-loaded liposomes showed promising respirable fractions, in contrast to zirconyl hydrogen phosphate nanocontainers. ... mehr

Verlagsausgabe §
DOI: 10.5445/IR/1000134294
Veröffentlicht am 26.06.2021
DOI: 10.1007/s13346-021-01011-7
Zitationen: 19
Zitationen: 18
Cover der Publikation
Zugehörige Institution(en) am KIT Institut für Anorganische Chemie (AOC)
Publikationstyp Zeitschriftenaufsatz
Publikationsjahr 2021
Sprache Englisch
Identifikator ISSN: 2190-393X, 2190-3948
KITopen-ID: 1000134294
Erschienen in Drug Delivery and Translational Research
Verlag Springer
Band 11
Seiten 1766–1778
Vorab online veröffentlicht am 08.06.2021
Nachgewiesen in Web of Science
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