Preparation, characterization and in vitro cytotoxicity study of dronedarone hydrochloride inclusion complexes.

Autor: Marcolino AIP; PostGraduate Program in Pharmaceutical Sciences, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil., Macedo LB; PostGraduate Program in Pharmaceutical Sciences, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil., Nogueira-Librelotto DR; PostGraduate Program in Pharmaceutical Sciences, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil; Department of Industrial Pharmacy, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil., Fernandes JR; Department of Industrial Pharmacy, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil., Bender CR; Department of Chemistry, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil., Wust KM; Department of Chemistry, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil., Frizzo CP; Department of Chemistry, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil., Mitjans M; Department of Biochemistry and Physiology, Faculty of Pharmacy and Food Science, Universitat de Barcelona, Joan XXIII 27-31, 08028 Barcelona, Spain., Vinardell MP; Department of Biochemistry and Physiology, Faculty of Pharmacy and Food Science, Universitat de Barcelona, Joan XXIII 27-31, 08028 Barcelona, Spain., Rolim CMB; PostGraduate Program in Pharmaceutical Sciences, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil; Department of Industrial Pharmacy, Universidade Federal de Santa Maria, Av. Roraima 1000, 97105-900 Santa Maria, RS, Brazil. Electronic address: clarice.rolim@gmail.com.
Jazyk: angličtina
Zdroj: Materials science & engineering. C, Materials for biological applications [Mater Sci Eng C Mater Biol Appl] 2019 Jul; Vol. 100, pp. 48-61. Date of Electronic Publication: 2019 Feb 26.
DOI: 10.1016/j.msec.2019.02.097
Abstrakt: Dronedarone is a new antiarrhythmic drug for the treatment of atrial fibrillation. This study investigated the complexation of dronedarone hydrochloride with β‑cyclodextrin (β-CD) and 2‑hydroxypropil‑β‑CD (HP-β-CD) using three different techniques. The complexes in the solid state were characterized by DSC, TGA, PXRD, FT-IR, SEM and 1 H NMR, demonstrating the formation of the inclusion complexes and exhibiting different properties from the pure drug. Its aqueous solubility increased about 4.0-fold upon complexation with β-CD and HP-β-CD. The dissolution rate of the drug was notably improved in all tested physiological pH values from 1.2 to 6.8 in the presence of both cyclodextrins. Furthermore, an in vitro cytotoxic assay revealed that the inclusion complexes could reduce the cytotoxic effects of the drug on 3T3 cells. The overall results suggest that the inclusion complexes with β-CD and HP-β-CD may be potentially useful in the preparation of novel pharmaceutical formulations containing dronedarone hydrochloride.
(Copyright © 2019 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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