Formulation and Evaluation of Niosomal Drug Delivery System of Ketoprofen

K. Kar, P. Sudheer
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引用次数: 5

Abstract

Purpose: Targeted drug delivery systems are used to deliver drugs to specific areas in definite concentration. Ketoprofen, belongs to NSAID, has various side effects associated with oral administration and also has less rate of permeation through skin from topical formulations. With an intention to increase skin permeability of ketoprofen through the skin by the use of vesicular structures called niosomes this study was undertaken. Methodology: In this particular study, niosomes were prepared by thin film hydration technique and ether injection technique. A topical niosomal gel was prepared by incorporating niosomes into 2% carbopol gel. Findings: Formulations prepared by thin film hydration technique, using drug, tween 40 and cholesterol in a ratio of 1:1:1 resulted in better entrapment efficiency and vesicular size in comparison to ether injection method. Evaluation: The niosomal formulations were characterised for vesicle size distribution, SEM and zeta potential. The best formulation (F16) was selected on the basis of drug entrapment efficiency of 83.63 ± 0.11% and in vitro diffusion profile. Conclusion: A comparative ex-vivo permeation study of niosomal gel against marketed gel, 2.5% w/w gel on excised rat abdominal skin model indicateda two-fold increase in permeation in comparison to marketed gel and a three fold increase in permeation in comparison to 2.5% w/w ketoprofen gel formula.
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酮洛芬乳质体给药系统的研制与评价
目的:靶向给药系统用于将药物以一定浓度递送到特定区域。酮洛芬属于非甾体抗炎药,口服给药有各种副作用,而且外用制剂通过皮肤的渗透率也较低。为了增加酮洛芬通过皮肤的渗透性,我们进行了一项研究,目的是利用一种叫做乳小体的囊泡结构。方法:采用薄膜水化技术和乙醚注射技术制备乳质体。将乳质体掺入2%卡波醇凝胶制备外用乳质体凝胶。结果:以药物、tween 40和胆固醇按1:1:1的比例采用薄膜水化技术制备的制剂比乙醚注射法具有更好的包封效率和囊泡大小。评价:用囊泡大小分布、扫描电镜和ζ电位对乳质体配方进行了表征。以药物包封率(83.63±0.11%)和体外扩散曲线为基础,优选出最佳处方(F16)。结论:通过对niosomal gel与市售gel的离体渗透研究,2.5% w/w凝胶在切除大鼠腹部皮肤模型上的渗透性比市售凝胶增加了2倍,比2.5% w/w酮洛芬凝胶配方的渗透性增加了3倍。
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