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首页> 外文期刊>Journal of Young Pharmacists >Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles
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Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles

机译：孟鲁司特钠固体脂质纳米粒的制备与评价

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Solid lipid nanoparticles (SLNs) are an alternative carrier system used to load the drug for targeting, to improve the bioavailability by increasing its solubility, and protecting the drug from presystemic metabolism. The avoidance of presystemic metabolism is due to the nano-metric size range, so that the liver cannot uptake the drug from the delivery system and is not metabolized by the liver. Montelukast sodium is an anti-asthmatic drug, because of its poor oral bioavailability, presystemic metabolism, and decreased half-life; it was chosen to formulate as the solid lipid nanoparticle (SLN) system by hot homogenization followed by an ultrasonication method, to overcome the above. Compritol ATO 888, stearic acid, and glyceryl monostearate were used as a lipid matrix and polyvinyl alcohol as a surfactant. The prepared formulations have been evaluated for entrapment efficiency, drug content, in vitro drug release, particle size analysis, scanning electron microscopy, Fourier transform-infrared studies (FT-IR), differential scanning calorimetry (DSC), and stability. Particle size analysis revealed that the SLN prepared from the higher melting point lipid showed a larger particle size and with increased carbon chain length of the fatty acids. Entrapment efficiency (EE) was ranging from 42% to 92%. In vitro release studies showed maximum cumulative drug release was obtained for F 1 (59.1%) containing stearic acid, and the lowest was observed for F 18 (28.1%) containing compritol ATO 888 after 12 h and all the formulations followed first-order release kinetics. FT-IR and DSC studies revealed no interaction between drug and lipids. Studies showed that increase in lipid concentration, increased particle size, EE, and maintained the sustained release of drug. Among all, compritol ATO 888 was chosen as the best lipid for formulating SLN because it had high EE and sustained the drug release.
机译：固体脂质纳米颗粒（SLN）是一种替代性载体系统，用于加载用于靶向的药物，通过增加其溶解度来提高生物利用度并保护药物免于系统前代谢。避免进行系统前代谢是由于纳米级的大小范围，因此肝脏无法从输送系统摄取药物并且不会被肝脏代谢。孟鲁司特钠是一种抗哮喘药，因为它的口服生物利用度差，全身代谢不足，半衰期缩短。为了克服上述问题，选择通过热均质然后超声处理来配制成固体脂质纳米颗粒（SLN）系统。使用Compritol ATO 888，硬脂酸和单硬脂酸甘油酯作为脂质基质，使用聚乙烯醇作为表面活性剂。已对所制备的制剂进行了包封效率，药物含量，体外药物释放，粒度分析，扫描电子显微镜，傅里叶变换红外研究（FT-IR），差示扫描量热法（DSC）和稳定性的评估。粒度分析显示，由较高熔点脂质制备的SLN显示出较大的粒度，并具有增加的脂肪酸碳链长度。包封率（EE）为42％至92％。体外释放研究表明，含有硬脂酸的F 1（59.1％）获得了最大的累积药物释放，而含有复合维生素ATO 888的F 18（28.1％）则获得了最低的累积药物释放，所有制剂均遵循一级释放动力学。 FT-IR和DSC研究表明药物与脂质之间没有相互作用。研究表明，脂质浓度增加，粒径，EE增加，并保持药物的持续释放。其中，由于Compeitol ATO 888具有较高的EE并能持续释放药物，因此被选为SLN配制的最佳脂质。

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