Preparation, optimization and characterization of controlled release mucoadhesive microspheres containing highly variable drug Itraconazole in reducing gastric variability as compared to innovator formulation 


By Yuvraj Singh Dangi, Kamta Prasad Namdeo 


Oral candidiasis is one of the most common, treatable oral mucosal infections seen in persons with human immunodeficiency virus (HIV) infection or acquired immune deficiency syndrome (AIDS). Oral candidiasis can be a frequent and significant source of oral discomfort, pain, loss of taste, and aversion to food. Candida albicans carriage and a history of oral candidiasis are other significant risk factors for oral candidiasis. For the normal healthy patient, the treatment of oral candidiasis is relatively simple and effective. Itraconazole (ITCZ), a poorly soluble drug is quiet effective in treatment of oral candidiasis. ITCZ belong to class IV of biopharmaceutical classification system and falls in category of highly variable drugs. A controlled release formulation of ITCZ has been developed in the form of mucoadhesive microspheres. A 32 factorial design has been constructed to extract best formulation. Parameters such as peppas model, hixon-crowell model, first order, zero order and matrix diffusion were studied. The optimized formulation was studied for pharmacokinetic behavior in terms of AUC, Cmax and tmax. The results shows that when the drug is released in a controlled manner the intra patient variability has been considerably reduced as compared to the drug released in immediate fashion. The Cmax, AUC and tmax for test and reference formulations was found to be 89 to 112.1 and 73.2 to 136.2, 79.9 to 106.4 and 81.6 to 141.4 and 90.1 to 118 and 68.3 to 88.4 respectively. 

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