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Itraconazole Niosomes Drug Delivery System and Its Antimycotic Activity against Candida albicans

DOI: 10.5402/2012/653465

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Abstract:

Niosomes have potential applications in topical drug delivery system. The objective of the study was to formulate and evaluate the niosome of Itraconazole. Surfactant?:?cholesterol ratio and quantity of ethanol used were studied by applying factorial design. Formulated niosomes were evaluated for vesicle size, entrapment efficiency, drug release, skin permeation, and antimycotic activity. Vesicle size, entrapment efficiency, and drug release were markedly dependent on surfactant?:?cholesterol ratio and quantity of ethanol used. Permeation of the drug through the skin was affected by cholesterol content in formulation. Itraconazole niosome were having larger zone of inhibition than marketed formulation when activity was checked against C. albicans. Niosomes may be a promising carrier for topical delivery of Itraconazole especially due to their simple production. 1. Introduction Most antifungal drug substances are lipophilic compounds, which are practically insoluble in water [1]. For skin care and the topical treatment of dermatological disease, a wide choice of vehicles ranging from solids to semisolids and liquid preparations is available to clinicians and patients [2]. Topical application of antimicrobial agents is a useful tool for the therapy of skin and soft-tissue infections [2]. A number of strategies to deliver antifungal using nanocarriers are developed to facilitate drug targeting infected cells. Nanosized carriers have been receiving special attention with the aim of minimizing the side effects and improving efficacy of drug therapy. Several nanosized delivery systems have already proved their effectiveness in antifungal therapy [3]. The total therapeutic effect of percutaneous preparations depends not only on the action of the drug itself, but also on other factors related to the structure of the vehicle. Taking into account the peculiarities of fungal parasites, the focus is placed particularly on lipid-based vehicles, and earlier studies have shown that results in improved antifungal activity [4]. Many techniques have been aimed to disrupt and weaken the highly organized intercellular lipids in an attempt to enhance drug transport across the intact skin; one of them is the vesicle formulation as skin delivery system [5–8]. Niosomes have been recognized as a good vehicles for the topical delivery of drugs [9]. They serve as “organic” solvent for the solubilization of poorly soluble drugs, for instances corticosteroids; as a result, higher local drug concentrations at the maximum thermodynamic activity can be applied. They may serve as a

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