Title :

High energy ball milling vs. nano spray drying in the development of supersaturated systems loaded with bosentan

Author(s) :

Krupa, Anna [Auteur]
Uniwersytet Jagielloński w Krakowie = Jagiellonian University [UJ]
Danede, Florence [Auteur]
Unité Matériaux et Transformations - UMR 8207 [UMET]
Majda, Dorota [Auteur]
Uniwersytet Jagielloński w Krakowie = Jagiellonian University [UJ]
Węgrzyn, Agnieszka [Auteur]
Uniwersytet Jagielloński w Krakowie = Jagiellonian University [UJ]
Strojewski, Dominik [Auteur]
Uniwersytet Jagielloński w Krakowie = Jagiellonian University [UJ]
Kondera, Ita [Auteur]
Uniwersytet Jagielloński w Krakowie = Jagiellonian University [UJ]
Willart, Jean-François [Auteur]
Unité Matériaux et Transformations (UMET) - UMR 8207

Journal title :

European Journal of Pharmaceutics and Biopharmaceutics

Abbreviated title :

European Journal of Pharmaceutics and Biopharmaceutics

Volume number :

188

Pages :

137-146

Publisher :

Elsevier BV

Publication date :

2023-07

ISSN :

0939-6411

English keyword(s) :

Bosentan
Supersaturation
Enabling formulations
Solvent evaporation
Mechanical activation
Poorly soluble drugs

HAL domain(s) :

Physique [physics]/Matière Condensée [cond-mat]/Science des matériaux [cond-mat.mtrl-sci]
Physique [physics]/Matière Condensée [cond-mat]/Matière Molle [cond-mat.soft]
Physique [physics]/Matière Condensée [cond-mat]/Systèmes désordonnés et réseaux de neurones [cond-mat.dis-nn]

English abstract : [en]

In this study, high energy ball milling and nano spray drying were used to prepare amorphous solid dispersions of bosentan in copovidone for the first time. In particular, the impact of this polymer on the bosentan ...
Show more >In this study, high energy ball milling and nano spray drying were used to prepare amorphous solid dispersions of bosentan in copovidone for the first time. In particular, the impact of this polymer on the bosentan amorphization kinetics was investigated. Copovidone was shown to facilitate the amorphization of bosentan upon ball milling. As a result, bosentan was dispersed in copovidone at the molecular level, forming amorphous solid dispersions, regardless of the ratio of the compounds. The similarity between the values of the adjustment parameter that describes the goodness of fit of the Gordon-Taylor equation to the experimental data (K = 1.16) and that theoretically calculated for an ideal mixture (K = 1.13) supported these findings. The kind of coprocessing method determined the powder microstructure and the release rate. The opportunity to prepare submicrometer-sized spherical particles using nano spray drying was an important advantage of this technology. Both coprocessing methods allowed the formation of long-lasting supersaturated bosentan solutions in the gastric environment with maximum concentrations reached ranging from four (11.20 μg/mL) to more than ten times higher (31.17 μg/mL) than those recorded when the drug was vitrified alone (2.76 μg/mL). Moreover, this supersaturation lasted for a period of time at least twice as long as that of the amorphous bosentan processed without copovidone (15 min vs. 30–60 min). Finally, these binary amorphous solid dispersions were XRD-amorphous for a year of storage under ambient conditions.Show less >

Language :

Anglais

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

Université de Lille
CNRS
INRAE
ENSCL

Collections :

• Unité Matériaux et Transformations (UMET) - UMR 8207

Research team(s) :

Matériaux Moléculaires et Thérapeutiques

Submission date :

2023-11-09T12:54:11Z
2023-11-10T09:14:44Z