Pregled bibliografske jedinice broj: 1203526
Investigation of praziquantel/cyclodextrin inclusion complexation
Investigation of praziquantel/cyclodextrin inclusion complexation // 20th International Symposium and Summer School on Bioanalysis : Book of Abstracts / Kilár, Ferenc ; Nagy, Laura (ur.).
Pečuh, 2022. str. 51-51 (pozvano predavanje, međunarodna recenzija, sažetak, znanstveni)
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Naslov
Investigation of praziquantel/cyclodextrin inclusion
complexation
Autori
Galić, Nives
Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni
Izvornik
20th International Symposium and Summer School on Bioanalysis : Book of Abstracts
/ Kilár, Ferenc ; Nagy, Laura - Pečuh, 2022, 51-51
Skup
20th International Symposium and Summer School on Bioanalysis
Mjesto i datum
Pečuh, Mađarska, 24.06.2022. - 30.06.2022
Vrsta sudjelovanja
Pozvano predavanje
Vrsta recenzije
Međunarodna recenzija
Ključne riječi
Praziquantel ; Cyclodextrins ; Inclusion complexes ; Stability studies ; Degradation products
Sažetak
Praziquantel (PZQ) is according to a biopharmaceutical classification system (BCS) class II anthelmintic drug characterized by poor solubility and a bitter taste, both of which can be efficiently solved by inclusion complexation with cyclodextrins (CDs). Both natural and chemically modified CDs can improve the in vitro dissolution properties, provide efficient taste- masking and/or alternative ways of drug delivery through inclusion complexation. In this work, a comprehensive investigation of praziquantel/cyclodextrin (PZQ/CD) complexes was conducted by means of UV-Vis spectroscopy, spectrofluorimetry, NMR spectroscopy, LC-HRMS/MS and molecular modelling. Phase solubility studies revealed that among four CDs tested, the randomly methylated β-CD ; RMβCD and the sulfobutylether sodium salt β-CD ; SBEβCD resulted in the highest increase in PZQ solubility (approximately 16- fold). The formation of 1:1 inclusion complexes was confirmed by HRMS, NMR and molecular modelling. Both cyclohexane and the central pyrazino ring, as well as an aromatic part of PZQ are included into the CD central cavity through several different binding modes, which exist simultaneously. Furthermore, the influence of CDs on PZQ stability was investigated in solution (HCl, NaOH, H2O2) and in the solid state (accelerated degradation, photostability) by UPLC- DAD/MS. Complexes in the solid state were prepared by grinding and analyzed as described previously.
Izvorni jezik
Engleski
Znanstvena područja
Kemija
