Formulation and evaluation of a novel mucoadhesive drug delivery system to treat intestinal candidiasis in immunocompromised patients

The limited solubility, and therefore bioavailability, of the antimycotic drug,itraconazole, used for the treatment of intestinal Candidiasis in immunocompromisedindividuals, has been well documented. Therapeutic regimen in these patients mayinclude daily administration of multiple doses of various drugs. Hence, improving theresidence time of therapeutic agents, would ensure a high continuous concentration inthe body and help decrease the dosing frequency. In our current study, we haveinvestigated a novel method of drug delivery, developed by utilizing the concept ofmucoadhesiveness, for the sustained release of the drug, itraconazole. Mucoadhesivebeads were prepared using two natural polymers, isabghula husk and alginate. Theminimum inhibitory concentration of itraconazole for Candida was found to be1.5milligram per millilitre. Accordingly, beads were prepared by ionic gelation methodusing calcium chloride as a crosslinking agent. Marked improvement in solubility of thedrug was noted after entrapment. Prepared beads were subjected to various evaluationsincluding particle size, swelling behaviour and mucoadhesivity. At pH 7.4, goodmucoadhesive property was exhibited up to 7 hours. Maximum swelling of beads wasobserved at 4hours in phosphate buffer after which the beads showed slight erosion.Fresh cock intestinal mucosa was used to assess the sustained release of itraconazolefrom the drug loaded beads and the reduction in candidal cells adhering to the mucosawas verified by the viable count technique. The results of our present study indicate thatmucoadhesive intestinal retentive isabghula- alginate beads could represent a promisingvehicle for drug delivery and help improve therapeutic efficacy and patient compliancein the future.