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Preparation and characterization of minoxidil loaded nanostructured lipid carrier gel for effective treatment of alopecia

机译:米诺地尔负载型纳米结构脂质载体凝胶的制备及表征

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In the present work attempts have been made to prepare the nanostructured lipid carrier (NLC) gel, by using minoxidil, which is preferably used in case of Alopecia, i.e. baldness pattern as a effective drug. The nine different formulations of Minoxidil-NLC (NLC1-NLC9) were prepared using solid and liquid lipids with Cholesterol and Soya lecithin in different concentrations by the melt dispersion ultrasonication method. Properties of NLC1-NLC9 such as the particle size and its distribution, the scanning electron microscopy (SEM), the drug entrapment efficiency (EE), and the drug release behavior were investigated. The nanoparticulate dispersion was suitably gelled and characterized with respect to drug content, pH, spreadability, rheology, and in vitro release. Safety of the NLC-based gel was assessed using primary skin irritation studies. The formulated NLC3 was spherical in shape, with average particle size of 280nm, zeta potential of -42.40mV and entrapment efficiency of 86.09%. Differential Scanning Calorimeter (DSC) measurements revealed that imperfect crystallization occurred in the inner core of the NLC particles. The drug release behavior from the NLC displayed a biphasic drug release pattern with burst release at the initial stage followed by sustained release. These results indicated that the NLC3 is a suitable carrier of minoxidil with improved drug loading capacity and controlled drug release properties. It has been observed that NLC gel produces the gel with good consistency, homogeneity, spreadability and rheological behavior. The developed NLC-based gel showed faster onset and elicited prolonged activity up to 16h. The present study concluded that the NLC-based gel containing minoxidil dissolved in a mixture of solid lipid and liquid lipid in the nanoparticulate form helped us to attain the objective of faster onset yet prolonged action as evident from in vitro release.
机译:在目前的工作中,已经尝试通过使用米诺地尔来制备纳米结构的脂质载体(NLC)凝胶,米诺地尔优选在脱发的情况下使用,即脱发模式作为有效药物。通过熔融分散超声方法,使用固体和液体脂质与胆固醇和大豆卵磷脂以不同浓度制备了9种不同的米诺地尔NLC制剂(NLC1-NLC9)。研究了NLC1-NLC9的性质,例如粒径和分布,扫描电子显微镜(SEM),药物截留效率(EE)和药物释放行为。纳米颗粒分散体被适当地凝胶化,并且关于药物含量,pH,铺展性,流变性和体外释放进行表征。使用主要的皮肤刺激性研究评估了基于NLC的凝胶的安全性。配制的NLC3为球形,平均粒径为280nm,ζ电位为-42.40mV,捕获效率为86.09%。差示扫描量热仪(DSC)测量表明,不完全结晶发生在NLC颗粒的内核中。 NLC的药物释放行为显示了一种双相药物释放模式,在初始阶段爆发性释放,然后持续释放。这些结果表明,NLC3是米诺地尔的合适载体,具有改善的载药量和受控的药物释放性能。已经观察到,NLC凝胶产生具有良好稠度,均质性,铺展性和流变行为的凝胶。已开发的基于NLC的凝胶显示起效更快,并引起长达16小时的延长活性。本研究得出结论,基于NLC的凝胶含有溶解在纳米脂质形式的固体脂质和液体脂质混合物中的米诺地尔,这有助于我们实现起效更快,作用延长的目标,这一点从体外释放中可以明显看出。

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