Pharmaceutics
Functional Pharmacological Validation of Betahistine Release from Chitosan Microspheres Using an Isolated Guinea-Pig Gastric Smooth-Muscle Model
Par Pilicheva B et Zagorchev P.
Contenu en anglais
Résumé
Background
Betahistine-loaded chitosan microspheres have previously demonstrated formulation-dependent drug release; however, conventional in vitro release testing does not establish whether the drug incorporated into the delivery system retains pharmacological activity.
Methods
This study evaluated the time-dependent functional activity of four previously characterized betahistine-loaded chitosan formulations using isolated guinea-pig gastric smooth muscle strips. Microsphere quantities corresponding to an equivalent nominal amount of 10 mg betahistine were compared with free betahistine. Spontaneous contractile activity was continuously recorded and mean peak contractile force (Favr) and the area under the Favr-time curve were evaluated.