基于聚乳酸羟乙酸共聚物的青蒿琥酯纳米颗粒的制备,及其抗疟活性和毒性评价（英文）

发布时间：2018-04-25 02:09

本文选题：青蒿琥酯-PLGA缓释系统 + 抗疟原虫　；参考：《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》2017年11期

【摘要】：目的:为疟疾治疗制定基于聚合物的青蒿琥酯纳米粒。创新点:以聚乳酸羟乙酸共聚物(PLGA)为载体,制备青蒿琥酯纳米颗粒。并以小鼠为模型,评估其抗疟疗效和安全性。方法:以PLGA为载体,采用从单一的水包油乳剂中进行溶剂蒸发的方法制备青蒿琥酯纳米颗粒。借助X射线衍射和差示扫描量热分析对纳米颗粒进行表征。以4 mg/kg的剂量对感染疟原虫的雄性瑞士白化小鼠进行体内抗疟活性的研究,测定血液和肝毒性的相关指标。体外实验以小鼠腹腔巨噬细胞细胞系RAW 264.7为模型,在7.8~1000μg/ml浓度范围内,测定游离型和包裹型青蒿琥酯的细胞毒性。结论:实验结果表明,纳米颗粒的粒径为(329.3±21.7)nm,包封率为(38.4±10.1)%。与游离青蒿琥酯(58.2%)相比,基于PLGA的青蒿琥酯纳米颗粒(Art-PLGA)具有较高的抑虫率(62.6%),P0.05。就血小板计数结果而言,对照组(305 000.00±148 492.40)明显地高于游离青蒿琥酯组(139 500.00±20 506.10)和Art-PLGA组(163 500.00±3535.53),P0.05。因此,药物的使用没有导致肝毒性的产生。体外细胞毒性试验结果表明,Art-PLGA的半数抑制浓度(IC50,468.0μg/ml)显著高于游离青蒿琥酯(7.3μg/ml),P0.05。基于PLGA的青蒿琥酯纳米颗粒是一种有效安全的抗疟治疗方法。
[Abstract]:Objective: to develop polymer-based artesunate nanoparticles for malaria treatment. Innovation: artesunate nanoparticles were prepared using poly (lactic acid) glycolic acid copolymer (PLGA) as the carrier. The antimalarial efficacy and safety were evaluated in mice. Methods: artesunate nanoparticles were prepared by solvent evaporation from a single oil-in-water emulsion using PLGA as carrier. The nanoparticles were characterized by X-ray diffraction and differential scanning calorimetry. The antimalarial activity of male Swiss albino mice infected with Plasmodium falciparum was studied at the dose of 4 mg/kg. The related indexes of blood and hepatotoxicity were determined. The mouse peritoneal macrophage cell line RAW 264.7 was used as a model in vitro. The cytotoxicity of artesunate free and encapsulated artesunate was measured in the concentration range of 7.81 渭 g/ml. Conclusion: the experimental results show that the particle size is 329.3 卤21.7 nm and the entrapment efficiency is 38.4 卤10.1 nm. Compared with free artesunate (58.2%), artesunate nanocrystalline artesunate (Art-PLGA) based on PLGA had a higher inhibition rate of 62.6% (P 0.05). The platelet count in the control group was 000.00 卤148,492.40), which was significantly higher than that in the free artesunate group (139 500.00 卤20 506.10) and Art-PLGA group (163 500.00 卤3 535.53 P0.05). Therefore, the use of drugs did not lead to hepatotoxicity. The results of cytotoxicity test in vitro showed that IC50468.0 渭 g / ml of Art-PLGA was significantly higher than that of free artesunate (7.3 渭 g / ml). Artesunate nanoparticles based on PLGA are an effective and safe antimalarial therapy.
【作者单位】： Department
【分类号】：R943;R965

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