Colon Targeting Drug - Synthesis and evaluation of prodrugs of Quiniodochlor by  -Glucosidase enzyme with HPLC methodology

Quiniodochlor has well established antimicrobial properties. It is used for treatment of amoebiasis caused by Entamoeba histolytica. The drug is to be delivered to the colon for its effective action against Entamoeba histolytica. But the pharmacokinetic profile of Quiniodochlor indicates that the drug is not completely and promptly absorbed after oral administration. Quiniodochlor is specifically targeted to colon by making its prodrugs. Chemical structure of Quiniodochlor posses a hydroxyl group which can be exploited to make glycosides through glycosidic conjugation. Prodrugs of Quiniodochlor were synthesized and their colon targeting evaluation by HPLC was done in order to deliver it specifically to colon for treatment of amoebiasis and other colonic diseases. Three prodrugs of quiniodochlor QG1, QG2, QG5 are synthesized and In vitro drug release studies of the synthesized glucosides in simulated GIT fluids containing &-glucosidase was done. The studies showed that these prodrugs hydrolyzed most rapidly in simulated ceacal fluid (0.1 M HCl, pH 1.2), rapidly in simulated intestinal fluid ( phosphate buffer, pH 7.4) and slowly in simulated gastric fluid (acetate buffer, pH 5.0).By comparing all the results with time period, it may be concluded that - Quiniodochlor Acetylated Glucoside (QG1) > Quiniodochlor Acetylated Galactoside (QG2) > Quiniodochlor Acetylated Xyloside (QG5) .The antiprotozoal activity is best for acetylated glucoside of quiniodochlor as compared to acetylated galactoside and xyloside.

Author(s): Gera Parul, Sharma S.K., Budhiraja Rajat

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