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Development of levosulpiride-loaded solid lipid nanoparticles and their in vitro and in vivo comparison with commercial product.
Journal of Microencapsulation ( IF 3.9 ) Pub Date : 2020-01-17 , DOI: 10.1080/02652048.2020.1713242
Nadra Khaleeq 1 , Fakhar-Ud Din 1 , Anam Sajjad Khan 1 , Samreen Rabia 1 , Junaid Dar 1 , Gul Majid Khan 1
Affiliation  

The aim of this study was to develop levosulpiride-loaded solid lipid nanoparticles (SLNs) with enhanced solubilisation and bioavailability. The levosulpiride loaded-SLNs were composed of levosulpiride, stearic acid, and tween 80 in their respective weight ratios of (1, 5, and 1.5 mg) dissolved in 1 ml distilled water. Physicochemical properties of the SLNs such as particle size, shape, crystallinity, and chemical interaction were evaluated. Further, the in vitro drug dissolution, pharmacokinetic and stability studies of the SLNs were performed. The SLNs were rounded shaped stable nanoparticles with average diameter of 200 nm. They demonstrate 1.5- and 3-fold better drug dissolution when compared with the commercial product and levosulpiride powder, respectively. The SLNs enhanced the bioavailability of levosulpiride 3 times and 7 times, respectively, when compared with the commercial product and levosulpiride powder. It can be concluded that SLNs are capable to improve the dissolution and bioavailability of levosulpiride, even more than the commercial product.

中文翻译:

负载左旋硫醚的固体脂质纳米颗粒的开发及其与市售产品的体内外比较。

这项研究的目的是开发具有增强的溶解度和生物利用度的负载左旋磺酰胺的固体脂质纳米颗粒(SLN)。负载左旋磺酰胺的SLNs由左旋磺酰胺,硬脂酸和吐温80组成,它们各自的重量比分别为(1、5和1.5 mg)溶于1 ml蒸馏水中。评估了SLN的理化性质,例如粒径,形状,结晶度和化学相互作用。此外,进行了SLNs的体外药物溶解,药代动力学和稳定性研究。SLN是平均直径为200 nm的圆形稳定纳米颗粒。与市售产品和左旋磺必利粉末相比,它们分别显示出1.5和3倍更好的药物溶出度。SLNs分别提高了levosulpiride的生物利用度3倍和7倍,当与市售产品和左旋磺必利粉末比较时。可以得出结论,SLNs能够改善左旋磺必利的溶出度和生物利用度,甚至比市售产品更高。
更新日期:2020-01-17
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