Titre :

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

Auteur(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

Titre de la revue :

European Journal of Pharmaceutics and Biopharmaceutics

Nom court de la revue :

European Journal of Pharmaceutics and Biopharmaceutics

Numéro :

188

Pagination :

137-146

Éditeur :

Elsevier BV

Date de publication :

2023-07

ISSN :

0939-6411

Mot(s)-clé(s) en anglais :

Bosentan
Supersaturation
Enabling formulations
Solvent evaporation
Mechanical activation
Poorly soluble drugs

Discipline(s) HAL :

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]

Résumé en anglais : [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 ...
Lire la suite >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.Lire moins >

Langue :

Anglais

Audience :

Internationale

Vulgarisation :

Non

Établissement(s) :

Université de Lille
CNRS
INRAE
ENSCL

Collections :

• Unité Matériaux et Transformations (UMET) - UMR 8207

Équipe(s) de recherche :

Matériaux Moléculaires et Thérapeutiques

Date de dépôt :

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