Liposomal form of erlotinib for local inhalation administration and efficiency of its transport to the lungs

0571764 - ÚPT 2024 RIV NL eng J - Journal Article
Szabová, J. - Mišík, O. - Fučík, J. - Mrázová, Kateřina - Mravcová, L. - Elcner, J. - Lízal, F. - Krzyžánek, Vladislav - Mravec, F.
Liposomal form of erlotinib for local inhalation administration and efficiency of its transport to the lungs.
International Journal of Pharmaceutics. Roč. 634, 5 March (2023), č. článku 122695. ISSN 0378-5173. E-ISSN 1873-3476
Research Infrastructure: Czech-BioImaging III - 90250
Institutional support: RVO:68081731
Keywords : Liposome * Non-small-cell lung cancer * Nebulization * Encapsulation * Aerodynamic particle size * Numerical simulations
OECD category: Electrical and electronic engineering
Impact factor: 5.8, year: 2022
Method of publishing: Limited access
https://www.sciencedirect.com/science/article/pii/S0378517323001151

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 approximate to 100 nm, zeta = 43 mV) even in the presence of polyethylene glycol (d approximate to 150 nm, zeta = 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 li-posomes nebulized by this nebulizer was lower than 2 % for all chosen vesicles.
Permanent Link: https://hdl.handle.net/11104/0344846