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采用电喷雾法制备、优化及评估聚乳酸-羟基乙酸共聚物/链激酶纳米粒

Preparation, Optimization and Activity Evaluation of PLGA/Streptokinase Nanoparticles Using Electrospray.

作者信息

Yaghoobi Nasrin, Faridi Majidi Reza, Faramarzi Mohammad Ali, Baharifar Hadi, Amani Amir

机构信息

Department of Medical Nanotechnology, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Adv Pharm Bull. 2017 Apr;7(1):131-139. doi: 10.15171/apb.2017.017. Epub 2017 Apr 13.

Abstract

PLGA nanoparticles (NPs) have been extensively investigated as carriers of different drug molecules to enhance their therapeutic effects or preserve them from the aqueous environment. Streptokinase (SK) is an important medicine for thrombotic diseases. In this study, we used electrospray to encapsulate SK in PLGA NPs and evaluate its activity. This is the first paper which investigates activity of an electrosprayed enzyme. Effect of three input parameters, namely, voltage, internal diameter of needle (nozzle) and concentration ratio of polymer to protein on size and size distribution (SD) of NPs was evaluated using artificial neural networks (ANNs). Optimizing the SD has been rarely reported so far in electrospray. From the results, to obtain lowest size of nanoparticles, ratio of polymer/enzyme and needle internal diameter (ID) should be low. Also, minimum SD was obtainable at high values of voltage. The optimum preparation had mean (SD) size, encapsulation efficiency and loading capacity of 37 (12) nm, 90% and 8.2%, respectively. Nearly, 20% of SK was released in the first 30 minutes, followed by cumulative release of 41% during 72 h. Activity of the enzyme was also checked 30 min after preparation and 19.2% activity was shown. Our study showed that electrospraying could be an interesting approach to encapsulate proteins/enzymes in polymeric nanoparticles. However, further works are required to assure maintaining the activity of the enzyme/protein after electrospray.

摘要

聚乳酸-羟基乙酸共聚物纳米颗粒(NPs)作为不同药物分子的载体已被广泛研究,以增强其治疗效果或使其免受水环境的影响。链激酶(SK)是治疗血栓性疾病的一种重要药物。在本研究中,我们使用电喷雾法将SK包裹在聚乳酸-羟基乙酸共聚物纳米颗粒中并评估其活性。这是第一篇研究电喷雾酶活性的论文。使用人工神经网络(ANNs)评估了三个输入参数,即电压、针头(喷嘴)内径和聚合物与蛋白质的浓度比对纳米颗粒大小和大小分布(SD)的影响。到目前为止,在电喷雾中很少有关于优化大小分布的报道。从结果来看,为了获得最小尺寸的纳米颗粒,聚合物/酶的比例和针头内径应该较低。此外,在高电压值下可获得最小的大小分布。最佳制剂的平均(SD)尺寸、包封率和载药量分别为37(12)nm、90%和8.2%。近20%的SK在最初30分钟内释放,随后在72小时内累积释放41%。在制备后30分钟也检测了酶的活性,显示有19.2%的活性。我们的研究表明,电喷雾可能是一种将蛋白质/酶包裹在聚合物纳米颗粒中的有趣方法。然而,需要进一步的工作来确保电喷雾后酶/蛋白质的活性得以维持。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c4/5426726/a67d36fb5774/apb-7-131-g001.jpg

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