engleski

High-resolution mass spectrometry characterization of cinnarizine – β-cyclodextrin inclusion complexes

Cinnarizine (CIN) is a piperazine derivative with antihistaminic and calcium channel blocking activity which is widely used for the treatment of vertigo and prevention of motion sickness. Due to its poor aqueous solubility, CIN is classified as a Class 2 drug substance according to The Biopharmaceutical Classification System [1]. It is known that cyclodextrins (CDs) can interact with poorly soluble drugs by forming inclusion and non- inclusion complexes and thus enhance drug aqueous solubility and bioavailability [2]. The aim of our study was to characterize complexes of CIN with natural β-CD and its hydroxypropyl (HPβCD) and randomly methylated (RMβCD) derivatives by electrospray ionization mass spectrometry (MS) since this technique can offer direct determination of CD inclusion complexes formation and their stoichiometry [3]. High- resolution quadrupole time-of-flight (Q-TOF) mass spectrometer system was used for obtaining MS spectra. In order to determine binding strength of the complexes, MS/MS experiments were performed. Corresponding collision energy breakdown curves were constructed and fragmentation schemes were suggested as well. REFERENCES [1] S. Raghuvanshi, K. Pathak, J. Drug Delivery 2014, 2014, 479246. [2] S. V. Kurkov, T. Loftsson, Int. J. Pharm. 2013, 453, 167–180. [3] M. Silion et al. in A. G. Woods, C. C. Darie (eds), Advancements of Mass Spectrometry in Biomedical Research, Adv. Exp. Med. Biol. 2019, 1140, 685–701.

cinnarizine ; cyclodextrin ; inclusion complexes ; mass spectrometry

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