Mesoporous particle-based microcontainers for intranasal delivery of imidazopyridine drugs.

ABSTRACT

The aim of this study was to develop mesoporous containers for entrapment of imidazopyridines, such as sedative-hypnotic medicine zolpidem, anxiolytic agent alpidem and their derivatives. For this purpose, calcium carbonate (size 1.2 µm (PDI 0.6), zeta potential -10 mV), manganese carbonate (2.5 µm (PDI 0.5), zeta potential -12 mV) and titanium dioxide particles (3.7 µm (PDI 0.4), zeta potential -15 mV) were used. The compounds were encapsulated applying two techniques adsorption on the preformed particles and co-precipitation during the synthesis of the particles. The polymer shell of the containers was formed by electrostatic adsorption of polyelectrolytes on the surface of the particles. The best encapsulation efficacy was shown for zolpidem incorporated into calcium carbonate (5.4%) and manganese carbonate (4.6%) by adsorption. Release of the compounds from the containers based on the proposed particles were characterised by the short time burst effect (<10 min) followed by desorption prolongation by formation of polymer shell. X-ray microtomography results demonstrate the prolonged retention of the containers with the mucoadhesive shell in the nasal cavity.