Albendazole, an effective broad-spectrum anthelmintic agent, showed
unpredictable therapeutic response caused by poor water solubility and
slow dissolution rate. Then, novel binary and multicomponent
supramolecular systems of two different solid forms of albendazole (I
and II) with maltodextrin alone or with glutamic acid were studied as an
alternative to improve the oral bioavailability of albendazole. The
interactions and effects on the properties of albendazole were studied
in solution and solid state. The solid systems were characterized using
Raman and Fourier transform-infrared spectroscopy, thermal analysis,
powder X-ray diffraction, and scanning electron microscopy. The
solubility measurements, performed in aqueous and simulated gastric
fluid, showed that albendazole (form II) was the most soluble form,
while its supramolecular systems showed the highest solubility in
simulated gastric fluid. On the other hand, the dissolution profiles of
binary and multicomponent systems in simulated gastric fluid displayed
pronounced increments of the dissolved drug and a faster dissolution
rate compared to those of free albendazole forms. Thus, these
supramolecular structures constitute an interesting alternative to
improve the physicochemical properties of albendazole, with potential
application for the preparation of pharmaceutical oral formulations.
%0 Journal Article
%1 WOS:000428932700047
%A Bongioanni, Agustina
%A Araujo, Bruno Sousa
%A de Oliveira, Yara Santiago
%A Longhi, Marcela R
%A Ayala, Alejandro
%A Garnero, Claudia
%C 233 SPRING ST, NEW YORK, NY 10013 USA
%D 2018
%I SPRINGER
%J AAPS PHARMSCITECH
%K acid; desmotrope; dissolution} glutamic maltodextrin; solubility; {albendazole;
%N 3
%P 1468-1476
%R 10.1208/s12249-018-0952-0
%T Improving Properties of Albendazole Desmotropes by Supramolecular
Systems with Maltodextrin and Glutamic Acid
%V 19
%X Albendazole, an effective broad-spectrum anthelmintic agent, showed
unpredictable therapeutic response caused by poor water solubility and
slow dissolution rate. Then, novel binary and multicomponent
supramolecular systems of two different solid forms of albendazole (I
and II) with maltodextrin alone or with glutamic acid were studied as an
alternative to improve the oral bioavailability of albendazole. The
interactions and effects on the properties of albendazole were studied
in solution and solid state. The solid systems were characterized using
Raman and Fourier transform-infrared spectroscopy, thermal analysis,
powder X-ray diffraction, and scanning electron microscopy. The
solubility measurements, performed in aqueous and simulated gastric
fluid, showed that albendazole (form II) was the most soluble form,
while its supramolecular systems showed the highest solubility in
simulated gastric fluid. On the other hand, the dissolution profiles of
binary and multicomponent systems in simulated gastric fluid displayed
pronounced increments of the dissolved drug and a faster dissolution
rate compared to those of free albendazole forms. Thus, these
supramolecular structures constitute an interesting alternative to
improve the physicochemical properties of albendazole, with potential
application for the preparation of pharmaceutical oral formulations.
@article{WOS:000428932700047,
abstract = {Albendazole, an effective broad-spectrum anthelmintic agent, showed
unpredictable therapeutic response caused by poor water solubility and
slow dissolution rate. Then, novel binary and multicomponent
supramolecular systems of two different solid forms of albendazole (I
and II) with maltodextrin alone or with glutamic acid were studied as an
alternative to improve the oral bioavailability of albendazole. The
interactions and effects on the properties of albendazole were studied
in solution and solid state. The solid systems were characterized using
Raman and Fourier transform-infrared spectroscopy, thermal analysis,
powder X-ray diffraction, and scanning electron microscopy. The
solubility measurements, performed in aqueous and simulated gastric
fluid, showed that albendazole (form II) was the most soluble form,
while its supramolecular systems showed the highest solubility in
simulated gastric fluid. On the other hand, the dissolution profiles of
binary and multicomponent systems in simulated gastric fluid displayed
pronounced increments of the dissolved drug and a faster dissolution
rate compared to those of free albendazole forms. Thus, these
supramolecular structures constitute an interesting alternative to
improve the physicochemical properties of albendazole, with potential
application for the preparation of pharmaceutical oral formulations.},
added-at = {2022-05-23T20:00:14.000+0200},
address = {233 SPRING ST, NEW YORK, NY 10013 USA},
author = {Bongioanni, Agustina and Araujo, Bruno Sousa and de Oliveira, Yara Santiago and Longhi, Marcela R and Ayala, Alejandro and Garnero, Claudia},
biburl = {https://www.bibsonomy.org/bibtex/2e7b8b54f0b57d3a6816a0c9057b949eb/ppgfis_ufc_br},
doi = {10.1208/s12249-018-0952-0},
interhash = {7d9658aa9fabaff51504a1f6173754ec},
intrahash = {e7b8b54f0b57d3a6816a0c9057b949eb},
issn = {1530-9932},
journal = {AAPS PHARMSCITECH},
keywords = {acid; desmotrope; dissolution} glutamic maltodextrin; solubility; {albendazole;},
number = 3,
pages = {1468-1476},
publisher = {SPRINGER},
pubstate = {published},
timestamp = {2022-05-23T20:00:14.000+0200},
title = {Improving Properties of Albendazole Desmotropes by Supramolecular
Systems with Maltodextrin and Glutamic Acid},
tppubtype = {article},
volume = 19,
year = 2018
}