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

Abstract

The limited solubility, and therefore bioavailability, of the antimycotic drug, itraconazole, used for the treatment of intestinal Candidiasis in immunocompromised individuals, has been well documented. Therapeutic regimen in these patients may include daily administration of multiple doses of various drugs. Hence, improving the residence time of therapeutic agents, would ensure a high continuous concentration in the body and help decrease the dosing frequency. In our current study, we have investigated a novel method of drug delivery, developed by utilizing the concept of mucoadhesiveness, for the sustained release of the drug, itraconazole. Mucoadhesive beads were prepared using two natural polymers, isabghula husk and alginate. The minimum inhibitory concentration of itraconazole for Candida was found to be 1.5milligram per millilitre. Accordingly, beads were prepared by ionic gelation method using calcium chloride as a crosslinking agent. Marked improvement in solubility of the drug was noted after entrapment. Prepared beads were subjected to various evaluations including particle size, swelling behaviour and mucoadhesivity. At pH 7.4, good mucoadhesive property was exhibited up to 7 hours. Maximum swelling of beads was observed at 4hours in phosphate buffer after which the beads showed slight erosion. Fresh cock intestinal mucosa was used to assess the sustained release of itraconazole from the drug loaded beads and the reduction in candidal cells adhering to the mucosa was verified by the viable count technique. The results of our present study indicate that mucoadhesive intestinal retentive isabghula- alginate beads could represent a promising vehicle for drug delivery and help improve therapeutic efficacy and patient compliance in the future.