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Titel: Spray-dried lactose-leucine microparticles for pulmonary delivery of antimycobacterial nanopharmaceuticals
VerfasserIn: Thiyagarajan, Durairaj
Huck, Benedikt
Nothdurft, Birgit
Koch, Marcus
Rudolph, David
Rutschmann, Mark
Feldmann, Claus
Hozsa, Constantin
Furch, Marcus
Besecke, Karen F. W.
Gieseler, Robert K.
Loretz, Brigitta
Lehr, Claus-Michael
Sprache: Englisch
Titel: Drug Delivery and Translational Research : an official journal of the Controlled Release Society
Bandnummer: 11
Heft: 4
Startseite: 1766
Endseite: 1778
Verlag/Plattform: Springer
Erscheinungsjahr: 2021
Dokumenttyp: Journalartikel / Zeitschriftenartikel
Abstract: 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. While the colloidal stability of silica NPs was improved after spray drying, MPs encapsulating either BTZ nanosuspensions or LVX-loaded liposomes showed the highest respirable fractions and active pharmaceutical ingredient loads. Importantly, for the BTZ nanosuspension, biocompatibility and in vitro uptake by a macrophage model cell line were improved even further after spray drying.
DOI der Erstveröffentlichung: 10.1007/s13346-021-01011-7
URL der Erstveröffentlichung: https://link.springer.com/article/10.1007/s13346-021-01011-7
Link zu diesem Datensatz: hdl:20.500.11880/31557
http://dx.doi.org/10.22028/D291-34431
ISSN: 2190-3948
2190-393X
Datum des Eintrags: 23-Jul-2021
Fakultät: NT - Naturwissenschaftlich- Technische Fakultät
Fachrichtung: NT - Pharmazie
Professur: NT - Prof. Dr. Claus-Michael Lehr
Sammlung:SciDok - Der Wissenschaftsserver der Universität des Saarlandes

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