Encapsulation of finasteride with native and modified γ-cyclodextrins. Extensive characterization of the complexes.

Autor: González-Louzao R; Universidad Católica San Antonio de Murcia (UCAM), Campus de los Jerónimos, N° 135, Guadalupe, 30107 Murcia, Spain., Lucas-Abellán C; Dpto. Tecnología Alimentaria y Nutrición, Universidad Católica San Antonio de Murcia (UCAM), Campus de los Jerónimos, N° 135, Guadalupe, 30107 Murcia, Spain., Pérez-Sánchez H; Bioinformatics and High Performance Computing Research Group (BIO-HPC), Dpto. Ciencias Politécnicas, Universidad Católica San Antonio de Murcia (UCAM), Campus de los Jerónimos, N° 135, Guadalupe, 30107 Murcia, Spain., Pedro Cerón-Carrasco J; Bioinformatics and High Performance Computing Research Group (BIO-HPC), Dpto. Ciencias Politécnicas, Universidad Católica San Antonio de Murcia (UCAM), Campus de los Jerónimos, N° 135, Guadalupe, 30107 Murcia, Spain., Antonio Gabaldón J; Dpto. Tecnología Alimentaria y Nutrición, Universidad Católica San Antonio de Murcia (UCAM), Campus de los Jerónimos, N° 135, Guadalupe, 30107 Murcia, Spain., López-Miranda S; Dpto. Tecnología Alimentaria y Nutrición, Universidad Católica San Antonio de Murcia (UCAM), Campus de los Jerónimos, N° 135, Guadalupe, 30107 Murcia, Spain., Josefa Yáñez-Gascón M; Dpto. Tecnología Alimentaria y Nutrición, Universidad Católica San Antonio de Murcia (UCAM), Campus de los Jerónimos, N° 135, Guadalupe, 30107 Murcia, Spain., Asín-Llorca M; AyC184, S.L., C/ Aequipa 1, planta 5ª, 28043 Madrid, Spain., Núñez-Delicado E; Dpto. Tecnología Alimentaria y Nutrición, Universidad Católica San Antonio de Murcia (UCAM), Campus de los Jerónimos, N° 135, Guadalupe, 30107 Murcia, Spain. Electronic address: enunez@ucam.edu.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2020 Sep 25; Vol. 587, pp. 119619. Date of Electronic Publication: 2020 Jul 18.
DOI: 10.1016/j.ijpharm.2020.119619
Abstrakt: The aim of this work was to study the complexation process of FIN with native and modified CDs, to develop an aqueous solution for the topical treatment of male androgenic alopecia. The effect of pH and temperature in the complexation process were studied by solubility studies. The complexes FIN-CDs were characterized by 1 HNMR and 2-D NMR (ROESY) spectroscopy. Molecular modeling studies and NMR data were used to build three-dimensional models of the complexes. FTIR, DSC and SEM techniques were also applied to strengthen physicochemical characterization, geometry as well as structural aspects evidencing the effective inclusion of FIN into the CDs' hydrophobic cavity. The most effective CDs in the FIN complexation were γ-CDs, and their modified HP-γ- and methyl-γ-CDs by forming 1:1 complexes. The Kc value obtained for γ-CDs was 9687 ± 51 M -1 , whereas the Kc values obtained for HP-γ- and methyl-γ-CDs were lower, indicating that the presence of HP or methyl groups hinder the entry of FIN in the hydrophobic cavity of γ-CDs. In conclusion, FIN aqueous solubility could be increased by complexation with CDs and the aqueous solutions obtained can be used to improve FIN therapeutic possibilities in a pleasant preparation for the patient that guarantees the adherence to the treatment.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2020 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE