Novel albendazole-glucan particles for enhancing intestinal absorption and improving hepatic targeting.

BACKGROUND

Glucan particles (GPs) are derived from the Saccharomyces cerevisiae cell wall. The hollow particles composed of β-1,3-D-glucan have been extensively studied in terms of immune regulation and macrophage-targeted drug delivery. Albendazole (ABZ) is a benzimidazole drug with good anti-parasitic activity and is the drug recommended by the World Health Organization for the first-line treatment of hydatid disease.

METHODS

A dynamic light scatterometer, scanning electron microscope, and transmission electron microscope were used to characterize the ABZ-GPs. High-performance liquid chromatography (HPLC), laser scanning confocal microscope (LSCM) and an in vivo small animal imaging system were used to evaluate theability of ABZ-GPs to be recognized by macrophages, whether ABZ-GPs are more readily absorbed and eliminated in the blood than the original ABZ drug in rats, and the ability of ABZ-GPs to target the mouse liver.

RESULTS

The ABZ-GPs were successfully constructed to achieve fluorescence, magnetic resonance imagining, and laser confocal microscopy imaging. The glucan shell effectively protects ABZ from enzymatic degradation and from being pumped out in the gastrointestinal tract. The analysis of ABZ and its major metabolite albendazole sulfoxide in the rat plasma and mouse liver showed that compared to the ABZ suspension group, the degradation of ABZ-GPSs in the blood was low, and the targeting of ABZ-GPSs in the liver was significantly enhanced.

CONCLUSIONS

In the oral treatment of hepatic hydatid disease, GPs can be used as carriers to achieve the targeted transport of ABZ, which in turn can be used for the targeted therapy of liver echinococcosis. Thus, ABZ-GPs may be a promising form of targeted therapy.