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Improving bioavailability and anthelmintic activity of albendazole by preparing albendazole-cyclodextrin complexes
J J García-Rodriguez1, J Torrado, F Bolás
1Departmento de Parasitología, Facultad de Farmacia, Universidad Complutense, Spain.
Parasite (Paris, France)
|August 4, 2001
Summary
Albendazole-cyclodextrin complexes (ABZ-CDC) show enhanced bioavailability and increased anthelmintic effects against Trichinella infections compared to albendazole suspensions. This novel formulation improves the efficacy of albendazole-sulphoxide (ABZSO) in treating parasitic worm infections.
Area of Science:
- Pharmacology and Parasitology
- Drug Delivery Systems
Background:
- Albendazole is a broad-spectrum anthelmintic drug.
- Albendazole's efficacy can be limited by its bioavailability.
- Trichinella spiralis infections pose a significant parasitic health concern.
Purpose of the Study:
- To compare the bioavailability and anthelmintic activity of albendazole-cyclodextrin complexes (ABZ-CDC) against albendazole suspensions (ABZ-CMC).
- To evaluate the efficacy of ABZ-CDC and ABZ-CMC against different life stages of Trichinella spiralis in a mouse model.
Main Methods:
- Experimental infection of Swiss CD-1 mice with Trichinella spiralis.
- Administration of ABZ-CDC and ABZ-CMC formulations orally at 50 mg/kg.
- Assessment of oral bioavailability and plasma concentrations of albendazole-sulphoxide (ABZSO) enantiomer (-).
- Evaluation of anthelmintic effects against enteral (adult worms) and parenteral (larvae) stages.
Main Results:
- ABZ-CDC demonstrated significantly increased oral bioavailability compared to ABZ-CMC.
- The anthelmintic effects against both adult worms and larvae were significantly enhanced with ABZ-CDC.
- Plasma concentrations of the active metabolite, albendazole-sulphoxide (ABZSO) enantiomer (-), were significantly higher following ABZ-CDC administration.
Conclusions:
- Albendazole-cyclodextrin complexes represent an improved drug delivery system for albendazole.
- ABZ-CDC significantly enhances the bioavailability and therapeutic efficacy against Trichinella infections.
- This formulation holds promise for more effective treatment of parasitic worm diseases.