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利用超临界二氧化碳萃取法制备吡喹酮固体脂质纳米粒:理化性质表征、释放特性和细胞毒性。

Praziquantel-Solid Lipid Nanoparticles Produced by Supercritical Carbon Dioxide Extraction: Physicochemical Characterization, Release Profile, and Cytotoxicity.

机构信息

Laboratory of Nanotechnology and Nanomedicine, Institute of Technology and Research, Aracaju, SE 49032-490, Brazil.

School of Pharmacy, University Tiradentes, Aracaju, SE 49032-490, Brazil.

出版信息

Molecules. 2019 Oct 28;24(21):3881. doi: 10.3390/molecules24213881.

Abstract

Solid lipid nanoparticles (SLNs) can be produced by various methods, but most of them are difficult to scale up. Supercritical fluid (SCF) is an important tool to produce micro/nanoparticles with a narrow size distribution and high encapsulation efficiency. The aim of this work was to produce cetyl palmitate SLNs using SCF to be loaded with praziquantel (PZQ) as an insoluble model drug. The mean particle size (nm), polydispersity index (PdI), zeta potential, and encapsulation efficiency (EE) were determined on the freshly prepared samples, which were also subject of Differential Scanning Calorimetry (DSC), Fourier-Transform Infrared Spectroscopy (FTIR), drug release profile, and in vitro cytotoxicity analyses. PZQ-SLN exhibited a mean size of ~25 nm, PdI ~ 0.5, zeta potential ~-28 mV, and EE 88.37%. The DSC analysis demonstrated that SCF reduced the crystallinity of cetyl palmitate and favored the loading of PZQ into the lipid matrices. No chemical interaction between the PZQ and cetyl palmitate was revealed by FTIR analysis, while the release or PZQ from SLN followed the Weibull model. PZQ-SLN showed low cytotoxicity against fibroblasts cell lines. This study demonstrates that SCF may be a suitable scale-up procedure for the production of SLN, which have shown to be an appropriate carrier for PZQ.

摘要

固体脂质纳米粒 (SLNs) 可以通过多种方法制备,但大多数方法难以放大。超临界流体 (SCF) 是一种重要的工具,可以制备具有窄粒径分布和高包封效率的微/纳米颗粒。本工作旨在使用 SCF 制备棕榈酸鲸蜡酯 SLNs,并用其负载吡喹酮 (PZQ) 作为难溶性模型药物。在新鲜制备的样品上测定了平均粒径 (nm)、多分散指数 (PdI)、Zeta 电位和包封效率 (EE),还进行了差示扫描量热法 (DSC)、傅里叶变换红外光谱 (FTIR)、药物释放曲线和体外细胞毒性分析。PZQ-SLN 的平均粒径约为 25nm,PdI 约为 0.5,Zeta 电位约为-28mV,EE 为 88.37%。DSC 分析表明,SCF 降低了棕榈酸鲸蜡酯的结晶度,有利于 PZQ 载入脂质基质中。FTIR 分析表明 PZQ 和棕榈酸鲸蜡酯之间没有化学相互作用,而 PZQ 从 SLN 中的释放遵循 Weibull 模型。PZQ-SLN 对成纤维细胞系的细胞毒性较低。本研究表明,SCF 可能是 SLN 生产的合适放大工艺,SLN 已被证明是 PZQ 的合适载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a59d/6864877/114978a816e2/molecules-24-03881-g001.jpg

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