Naslov
Mechanochemical activation of dasatinib to improve its oral absorption properties in the treatment of leukemia

Autori
Sokač, Katarina ; Žižek, Krunoslav

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Solid-State Science & Research - Book of Abstracts / Biliškov, Nikola ; Karadeniz, Bahar ; Pantalon Juraj, Natalija - Zagreb : Institut Ruđer Bošković, 2023, 86-86

ISBN
978-953-7941-48-2

Skup
Solid-State Science & Research

Mjesto i datum
Zagreb, Hrvatska, 28.06.2023. - 30.06.2023

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
dasatinib ; mechanochemical activation ; polyvinylpyrrolidone ; amorphous solid dispersion ; tablet

Sažetak
Dasatinib (DAS) is a second-generation tyrosine kinase inhibitor used for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia and acute lymphoblastic leukemia. However, this drug is characterized by poor gastrointestinal absorption and low bioavailability due to its low aqueous solubility. A promising approach to improve the properties of DAS is to modify its crystalline structure by supramolecular structural modifications, such as the preparation of a co-amorphous system. This research is focused on the application of the green co-grinding method to prepare amorphous solid dispersions of DAS in a matrix of polyvinylpyrrolidone (PVP). Several favorable events were expected: a reduction in the particle size of the drug and thus an increase in the specific surface area, better wettability, and possible intermolecular interactions between DAS and PVP, which could also improve the dissolution rate of the drug and thus its bioavailability. Amorphous solid dispersions and fluidized bed melt granulation were used to prepare tablets with strictly defined aimed properties. In vitro dissolution tests confirmed that this particular drug could be mechanochemically activated in terms of improving its dissolution properties.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Kemijsko inženjerstvo

POVEZANOST RADA