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Liposomal form of erlotinib for local inhalation administration and efficiency of its transport to the lungs
J. Szabová, O. Mišík, J. Fučík, K. Mrázová, L. Mravcová, J. Elcner, F. Lízal, V. Krzyžánek, F. Mravec
Jazyk angličtina Země Nizozemsko
Typ dokumentu časopisecké články
- MeSH
- aplikace inhalační MeSH
- bronchodilatancia MeSH
- erlotinib MeSH
- lékové transportní systémy MeSH
- lidé MeSH
- liposomy MeSH
- nádory plic * MeSH
- nebulizátory a vaporizátory MeSH
- nemalobuněčný karcinom plic * MeSH
- plíce MeSH
- respirační aerosoly a kapénky MeSH
- velikost částic MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
This contribution is focused on the preparation of a liposomal drug delivery system of erlotinib resisting the nebulization process that could be used for local treatment of non-small-cell lung cancer. Liposomes with different compositions were formulated to reveal their influence on the encapsulation efficiency of erlotinib. An encapsulation efficiency higher than 98 % was achieved for all vesicles containing phosphatidic acid (d ≈ 100 nm, ζ = - 43 mV) even in the presence of polyethylene glycol (d ≈ 150 nm, ζ = - 17 mV) which decreased this value in all other formulas. The three most promising formulations were nebulized by two air-jet and two vibrating mesh nebulizers, and the aerosol deposition in lungs was calculated by tools of computational fluid and particle mechanics. According to the numerical simulations and measurements of liposomal stability, air-jet nebulizers generated larger portion of the aerosol able to penetrate deeper into the lungs, but the delivery is likely to be more efficient when the formulation is administered by Aerogen Solo vibrating mesh nebulizer because of a higher portion of intact vesicles after the nebulization. The leakage of encapsulated drug from liposomes nebulized by this nebulizer was lower than 2 % for all chosen vesicles.
Faculty of Mechanical Engineering Brno University of Technology Brno Czech Republic
Institute of Scientific Instruments of the Czech Academy of Sciences v v i Brno Czech Republic
Materials Research Centre Faculty of Chemistry Brno University of Technology Brno Czech Republic
Citace poskytuje Crossref.org
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- $a This contribution is focused on the preparation of a liposomal drug delivery system of erlotinib resisting the nebulization process that could be used for local treatment of non-small-cell lung cancer. Liposomes with different compositions were formulated to reveal their influence on the encapsulation efficiency of erlotinib. An encapsulation efficiency higher than 98 % was achieved for all vesicles containing phosphatidic acid (d ≈ 100 nm, ζ = - 43 mV) even in the presence of polyethylene glycol (d ≈ 150 nm, ζ = - 17 mV) which decreased this value in all other formulas. The three most promising formulations were nebulized by two air-jet and two vibrating mesh nebulizers, and the aerosol deposition in lungs was calculated by tools of computational fluid and particle mechanics. According to the numerical simulations and measurements of liposomal stability, air-jet nebulizers generated larger portion of the aerosol able to penetrate deeper into the lungs, but the delivery is likely to be more efficient when the formulation is administered by Aerogen Solo vibrating mesh nebulizer because of a higher portion of intact vesicles after the nebulization. The leakage of encapsulated drug from liposomes nebulized by this nebulizer was lower than 2 % for all chosen vesicles.
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