Abstract

Niosomes or non-ionic surfactants vesicles are microscopic lamellar structures formed on the admixture of a non-ionic surfactant, cholesterol and stearylamine with subsequent hydration in aqueous media. The delivery of drugs by “vesicular drug delivery system” such as niosomes provides several important advantages over conventional drug therapy. Diacerein is an Interleukin-1 inhibitor and it is highly effective in relieving the symptoms of osteoarthritis. Diacerein, in contrast to NSAIDs, are potent inhibitor of IL-1 beta induced nitric oxide production by chondrocytes and cartilage, without reducing prostaglandin E2 production. The main objective of this study was to design suitable niosome-encapsulated drug delivery for anti-inflammatory drugs like Diacerein and evaluate the vesicle size, entrapment efficiency, in vitro release and physical stability of the system. Non-ionic surfactants used were Tween (40&60), cholesterol and stearylamine in molar ratio 1:1:0.1. The niosomes were prepared by thin film hydration method. The higher entrapment efficiency was observed with niosome (F11) prepared from tween 60, cholesterol and 2.5 min sonication. The release pattern shown by these formulations were first order & Higuchi diffusion controlled mechanism. The physical stability study show that niosomal preparation stored at refrigerated temperature for 60 days show maximum drug retained compare to room temperature and elevated temperature conditions. Finding of all this investigation conclusively demonstrate prolongation of drug release at a constant and controlled rate after niosomal encapsulation of Diacerein.

Highlights

  • The basic goal of drug therapy is to achieve a steady state blood or tissue level that is therapeutically effective and nontoxic for an extended period

  • The photomicrograph of Diacerein niosomes prepared by thin film hydration method is shown in figure (1)

  • The means particle diameters of niosomes, composed of tween 40 and 60 with cholesterol are shown in table (2)

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Summary

Introduction

The basic goal of drug therapy is to achieve a steady state blood or tissue level that is therapeutically effective and nontoxic for an extended period. Novel drug delivery systems aim to deliver the drug at a rate directed by the needs of the body during the period of treatment and channel the active entity to the site of action (Biju et al, 2006). Targeted drug delivery implies for selective and effective localization of pharmacologically active moiety at preidentified (preselected) targeted (s) in therapeutic concentration while restricting its access to nontarget normal cellular linings minimizing toxic effects and maximizing therapeutic index. Targeted drug delivery is an event where a drug carrier complex/conjugate delivers drug (s) exclusively to the preselected targeted cells in a specific manner (Vyas and Khar, 2004). To pursue optical drug action, functional molecules could be transported by a carrier to the site of action and released to perform their task (Shahiwala and Misra, 2002)

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