Abstract
Albendazole is a benzimidazole carbamate extensively used in oral chemotherapy against intestinal parasites, due to its broad spectrum activity, good tolerance and low cost. However, the drug has the disadvantage of poor bioavailability due to its very low solubility in water; as a consequence, a very active area of research focuses on the development of new pharmaceutical formulations to increase its solubility, dissolution rate, and bioavailability. The primary objective of this study was to prepare randomly methylated β-cyclodextrins inclusion complexes to increase albendazole dissolution rate, in order to enhance its antiparasitic activity. This formulation therapeutic efficacy was contrasted with that of the pure drug by treating Trichinella spiralis infected mice during the intestinal phase of the parasite cycle, on days five and six post-infection. This protocol significantly decreased muscle larval burden measured in the parenteral stage on day 30 post-infection, when compared with the untreated control. Thus, it could be demonstrated that the inclusion complexes improve the in vivo therapeutic activity of albendazole.
Highlights
Trichinellosis is a foodborne parasitic zoonosis widely distributed all over the world in most climates, except for deserts, with a burden of approximately 10,000 people per year and a 0.2% mortality rate. [1] Humans acquire the infection by ingestion of undercooked meat contaminated with Trichinella spp
The Kf value obtained for the inclusion complex between ABZ and randomly methylated b-CD (RM-b-CD) was 336.70 M21 suggesting a stable complex in comparison with the Kf obtained with b-CD: 67.90 M21 and HP-b-CD: 313.16 M21
The physicochemical evaluation of the inclusion complexes prepared with ABZ and RM-b-CD showed promising results
Summary
Trichinellosis is a foodborne parasitic zoonosis widely distributed all over the world in most climates, except for deserts, with a burden of approximately 10,000 people per year and a 0.2% mortality rate. [1] Humans acquire the infection by ingestion of undercooked meat contaminated with Trichinella spp. The drug belongs to Class II in the Biopharmaceutics Classification System It is poorly water soluble and highly lipophilic (log P of 2.55) and, it can exhibit unfavourable bioavailability after oral administration, leading to variable oral absorption [5]. In this context, several formulation techniques have been previously investigated to increase ABZ dissolution rate, including solid dispersion, polymeric microencapsulation and complexation with cyclodextrins (CDs) [5,6,7,8,9,10,11,12]
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