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磷脂纳米颗粒的微流控制造:稳定性、包封效率和药物释放

Microfluidic manufacturing of phospholipid nanoparticles: Stability, encapsulation efficacy, and drug release.

作者信息

Guimarães Sá Correia Mariana, Briuglia Maria L, Niosi Fabio, Lamprou Dimitrios A

机构信息

Strathclyde Institute of Pharmacy and Biomedical Sciences (SIPBS), University of Strathclyde, 161 Cathedral Street, G4 0RE Glasgow, United Kingdom.

National EPSRC Centre for Innovative Manufacturing in Continuous Manufacturing and Crystallisation (CMAC), University of Strathclyde, Technology and Innovation Centre, 99 George Street, G1 1RD Glasgow, United Kingdom.

出版信息

Int J Pharm. 2017 Jan 10;516(1-2):91-99. doi: 10.1016/j.ijpharm.2016.11.025. Epub 2016 Nov 10.

Abstract

Liposomes have been the centre of attention in research due to their potential to act as drug delivery systems. Although its versatility and manufacturing processes are still not scalable and reproducible. In this study, the microfluidic method for liposomes preparation is presented. DMPC and DSPC liposomes containing two different lipid/cholesterol ratios (1:1 and 2:1) are prepared. Results from this preparation process were compared with the film hydration method in order to understand benefits and drawbacks of microfluidics. Liposomes characterisation was evaluated through stability studies, encapsulation efficacy and drug release profiles of hydrophilic and lipophilic compounds. Stability tests were performed during 3 weeks and the liposomes properties of the most stable formulations were determined using Infrared Microscopy and Atomic Force Microscopy. Microfluidic allows loading of drugs and assembly in a quick single step and the chosen flow ratio for liposomes formulation plays a fundamental role for particle sizes. One hydrophilic and one lipophilic compounds were incorporated showing how formulation and physic-chemical characteristics can influence the drug release profile.

摘要

脂质体因其作为药物递送系统的潜力而一直是研究的焦点。尽管其多功能性和制造工艺仍无法规模化和重现。在本研究中,介绍了用于制备脂质体的微流控方法。制备了含有两种不同脂质/胆固醇比例(1:1和2:1)的二肉豆蔻酰磷脂酰胆碱(DMPC)和二硬脂酰磷脂酰胆碱(DSPC)脂质体。将该制备过程的结果与薄膜水化法进行比较,以了解微流控技术的优缺点。通过稳定性研究、亲水性和亲脂性化合物的包封率及药物释放曲线对脂质体进行表征。稳定性测试进行了3周,并使用红外显微镜和原子力显微镜确定了最稳定制剂的脂质体性质。微流控技术允许在一个快速的单一步骤中加载药物并进行组装,并且用于脂质体制剂的选定流速比对于粒径起着至关重要的作用。掺入了一种亲水性化合物和一种亲脂性化合物,展示了制剂和物理化学特性如何影响药物释放曲线。

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