FORMULATION, DEVELOPMENT AND CHARACTERIZATION OF EFFECTIVE NIOSOMAL DRUG DELIVERY SYSTEM FOR THE TREATMENT OF DIABETES MELLITUS

Current Research in Pharmaceutical Sciences Pub Date : 2020-12-31 DOI:10.24092/crps.2020.100402

Nida Musheer, Vikrant Gupta

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Abstract

In the present study, gliclazide-loaded niosomes are formulated and evaluated for their in vitro as well as in vivo characteristic in an attempt to improve the oral bioavailability of the drug. Formulation of niosomes was optimized for highest percentage of drug entrapment. Microscopic observation confirmed that all particles were uniform in size and shape. The entrapment efficiency was determined by separating the unentrapped drug using dialysis. The in vitro release studies of drug from niosomes exhibited a prolonged drug release as observed over a period of 24 h. The positive values of zeta potential indicated that the gliclazide niosomes were stabilized by electrostatic repulsive forces. Results from stability study have shown that the drug leakage from the vesicles was least at 4ºC followed by 25 and 37ºC. The niosomes showing maximum entrapment and suitable release rate were selected for in vivo evaluation. In conclusion, the niosomal formulation could be a promising delivery system for gliclazide with improved bioavailability and prolonged drug release profile. KEYWORDS: Heme Oxygenase Inhibitor, HO-1, 2D QSAR, 3D QSAR, kNN-MFA

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治疗糖尿病的有效niosomal给药系统的研制与表征

在本研究中，为了提高药物的口服生物利用度，我们制定了格列齐特负载niosomes，并对其体外和体内特性进行了评估。以药物包封率最高为目标，优化了乳质体的配方。显微镜观察证实，所有的颗粒在大小和形状上都是均匀的。通过透析分离未包裹的药物来确定包裹效率。体外药物释放研究显示，在24小时的时间内，药物释放时间较长。zeta电位的阳性表明，格列齐特乳小体在静电斥力的作用下是稳定的。稳定性研究结果表明，药物在4℃时渗漏最少，其次是25℃和37℃。选择具有最大包裹度和合适释放率的乳质体进行体内评价。综上所述，niosomal制剂具有提高格列齐特生物利用度和延长药物释放时间的优点，是一种很有前景的给药系统。关键词:血红素加氧酶抑制剂，HO-1, 2D QSAR, 3D QSAR, kNN-MFA

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Current Research in Pharmaceutical Sciences

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