Naslov
Drug/cyclodextrin supramolecular complexes with enhanced functionality

Autori
Galić, Nives

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, neobjavljeni rad, znanstveni

Skup
59. savjetovanje SHD

Mjesto i datum
Novi Sad, Srbija, 01.06.2023. - 02.06.2023

Vrsta sudjelovanja
Plenarno

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
Cyclodextrins ; Praziquantel ; Nabumetone ; Inclusion complexes

Sažetak
To be pharmacologically active, all drugs must be soluble in water to some extent, and most of them should be lipophilic to penetrate biological membranes. The water solubility depends on the drug structure, but also on the drug formulation. Different technologies and methods are continuously developed to improve solubility of poorly soluble drugs, and one of them is inclusion of drugs into macrocycles such as cyclodextrins (CDs).1 CDs are cyclic oligomers composed of glucopyranose units that are connected through glycosidic 1, 4 bonds. Their structures resemble a truncated cone having a narrow rim, a wide rim and a cavity (Figure 1). Praziquantel (PZQ) and nabumetone (NAB) are according to a biopharmaceutical classification system (BCS) class II drugs which are characterized by good permeability and poor solubility. Due to their low aqueous solubility, large oral doses are required which can be efficiently solved by complexation of drugs with (CDs). The investigation of drug/cyclodextrin complexes were conducted by means of UV-Vis spectroscopy, spectrofluorimetry, calorimetry, LC-HRMS/MS, NMR spectroscopy and molecular modelling. The results obtained for PZQ and NAB complexes with beta- cyclodextrin and its derivatives, namely hydroxypropyl-beta-CD (HPCD), sulfobutylether- beta-CD (SBECD) and randomly methylated beta- cyclodextrin (RMCD) are pressented. The enhancement of aqueous solubility of both drugs was achieved. The formation of 1:1 inclusion complex was confirmed by HRMS, NMR and molecular modelling. 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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA