PHARMACOKINETICS OF ALBENDAZOLE ADMINISTERED ORALLY ALONG WITH QUERCETIN AS CHITOSAN-ALGINATE ENCAPSULATED MICROSPHERES IN BROILERS
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Date
2017-12
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SRI VENKATESWARA VETERINARY UNIVERSITY TIRUPATI - 517 502. (A.P.) INDIA
Abstract
ABSTRACT:
The present study was aimed to investigate the pharmacokinetics of albendazole administered orally along with quercetin as chitosan-alginate encapsulated microspheres in broilers. Thirty two adult broilers were divided into four groups with eight birds in each group and the treatment was given as follows: groups I and II received pure albendazole orally and intravenously @ 10 mg/kg respectively, while groups III and IV received albendazole @ 10 mg/kg in modified formulations of chitosan-alginate and chitosan-alginate with quercetin respectively. Blood was collected at various time intervals. Plasma was separated by centrifuging the blood and was subjected to HPLC assay for estimation of albendazole and albendazole sulphoxide. The pharmacokinetic parameters were analyzed by non-compartmental model. In group I that received pure albendazole orally ABZ could not be detected in the plasma at any point of time, while in other three groups ABZ was detectable up to 9-12 h after administration. The Cmax of ABZ in groups II and IV was significantly higher when compared to group III, while tmax was significantly higher in group IV when compared to groups II and III. The AUC observed in group IV was significantly (~2.5 fold) higher compared to groups II and III. The volume of distribution and clearance of ABZ in group IV was significantly lower when compared to groups II and III. Albendazole sulphoxide, the active metabolite of albendazole, could be detected from one hour to 48 h in group IV compared to 0.5 to 36 h in group I, 0.083 to 36 h in group II and 0.5 to 48 h in group III. The pharmacokinetics of ABZ-SO revealed a significantly higher t1/2 and maximum Cmax in groups III and IV when compared to group I. The AUC observed in group II, III and IV was significantly higher compared to group I though the AUC observed in group IV was non-significantly lower than that of group III. The MRT observed in group IV was longer than that observed in groups I and II. Similar to its parent compound ABZ-SO also showed similar trend with respect to Vd and clearance. The results in present study indicate that the quercetin has increased the absorption of ABZ and decreased its metabolite formation probably by inhibiting intestinal/hepatic CYPs. The modified formulations containing chitosan-alginate and quercetin prolonged the absorption and elimination of the active metabolite of ABZ-SO as evidenced by increased Cmax, AUC, and MRT observed in groups III and IV. Keeping in view of the enhanced absorption of albendazole and improved relative bioavailability of its active metabolite albendazole sulphoxide from microsphere formulations containing chitosan and quercetin, further appropriate studies can be performed to identify their efficacy in combatting systemic helminthic infections.
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