载青蒿素的 PC L-PEG-PCL 纳米粒的制备及其体内抗疟活性评价。
Preparation and in vivo evaluation of anti-plasmodial properties of artemisinin-loaded PCL-PEG-PCL nanoparticles.
机构信息
a Zanjan Pharmaceutical Biotechnology Research Center , Zanjan University of Medical Sciences , Zanjan , Iran.
b Department of Pharmaceutical Biotechnology, School of Pharmacy , Zanjan University of Medical Sciences , Zanjan , Iran.
出版信息
Pharm Dev Technol. 2018 Nov;23(9):911-920. doi: 10.1080/10837450.2017.1372781. Epub 2017 Sep 11.
PURPOSE
Artemisinin (ART) has anti-inflammatory, antimicrobial, antioxidant, anti-amyloid, and anti-malarial effects, but its application is limited due to its low water solubility and poor oral bioavailability. In this study, the bioavailability, water solubility, and anti-plasmodial property of ART were improved by PCL-PEG-PCL tri-block copolymers.
METHODS
The structure of the copolymers was characterized by H NMR, FT-IR, DSC, and GPC techniques. ART was encapsulated within micelles by a single-step nano-precipitation method, leading to the formation of ART-loaded PCL-PEG-PCL micelles. The obtained micelles were characterized by dynamic light scattering (DLS) and atomic force microscopy (AFM). The in vivo anti-plasmodial activity of ART-loaded micelles was measured against Plasmodium berghei infected Swiss albino mice.
RESULTS
The results showed that the zeta potential of ART-loaded micelles was about -8.37 mV and the average size was 91.87 nm. ART was encapsulated into PCL-PEG-PCL micelles with a loading capacity of 19.33 ± 0.015% and encapsulation efficacy of 87.21 ± 3.32%. In vivo anti-plasmodial results against P. berghei showed that multiple injections of ART-loaded micelles could prolong the circulation time and increase the therapeutic efficacy of ART.
CONCLUSION
These results suggested that PCL-PEG-PCL micelles would be a potential carrier for ART for the treatment of malaria.
目的
青蒿素（ART）具有抗炎、抗菌、抗氧化、抗淀粉样蛋白和抗疟原虫作用，但由于其水溶性低和口服生物利用度差，其应用受到限制。本研究通过聚己内酯-聚乙二醇-聚己内酯三嵌段共聚物提高了 ART 的生物利用度、水溶性和抗疟原虫特性。
方法
通过 H NMR、FT-IR、DSC 和 GPC 技术对共聚物的结构进行了表征。ART 通过单步纳米沉淀法包封在胶束中，形成载 ART 的 PCL-PEG-PCL 胶束。用动态光散射（DLS）和原子力显微镜（AFM）对所得胶束进行了表征。用载 ART 胶束对感染伯氏疟原虫的瑞士白化病小鼠进行体内抗疟原虫活性测定。
结果
结果表明，载 ART 胶束的zeta 电位约为-8.37 mV，平均粒径为 91.87 nm。ART 以载药量为 19.33±0.015%和包封率为 87.21±3.32%的形式被包封到 PCL-PEG-PCL 胶束中。对 P. berghei 的体内抗疟原虫结果表明，ART 载药胶束的多次注射可以延长循环时间并提高 ART 的治疗效果。
结论
这些结果表明，PCL-PEG-PCL 胶束可能是治疗疟疾的 ART 的潜在载体。
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