本文選題：青蒿琥酯-PLGA緩釋系統(tǒng) + 抗瘧原蟲　； 參考：《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》2017年11期

【摘要】：目的:為瘧疾治療制定基于聚合物的青蒿琥酯納米粒。創(chuàng)新點(diǎn):以聚乳酸羥乙酸共聚物(PLGA)為載體,制備青蒿琥酯納米顆粒。并以小鼠為模型,評估其抗瘧療效和安全性。方法:以PLGA為載體,采用從單一的水包油乳劑中進(jìn)行溶劑蒸發(fā)的方法制備青蒿琥酯納米顆粒。借助X射線衍射和差示掃描量熱分析對納米顆粒進(jìn)行表征。以4 mg/kg的劑量對感染瘧原蟲的雄性瑞士白化小鼠進(jìn)行體內(nèi)抗瘧活性的研究,測定血液和肝毒性的相關(guān)指標(biāo)。體外實(shí)驗(yàn)以小鼠腹腔巨噬細(xì)胞細(xì)胞系RAW 264.7為模型,在7.8~1000μg/ml濃度范圍內(nèi),測定游離型和包裹型青蒿琥酯的細(xì)胞毒性。結(jié)論:實(shí)驗(yàn)結(jié)果表明,納米顆粒的粒徑為(329.3±21.7)nm,包封率為(38.4±10.1)%。與游離青蒿琥酯(58.2%)相比,基于PLGA的青蒿琥酯納米顆粒(Art-PLGA)具有較高的抑蟲率(62.6%),P0.05。就血小板計(jì)數(shù)結(jié)果而言,對照組(305 000.00±148 492.40)明顯地高于游離青蒿琥酯組(139 500.00±20 506.10)和Art-PLGA組(163 500.00±3535.53),P0.05。因此,藥物的使用沒有導(dǎo)致肝毒性的產(chǎn)生。體外細(xì)胞毒性試驗(yàn)結(jié)果表明,Art-PLGA的半數(shù)抑制濃度(IC50,468.0μg/ml)顯著高于游離青蒿琥酯(7.3μg/ml),P0.05�；赑LGA的青蒿琥酯納米顆粒是一種有效安全的抗瘧治療方法。
[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 鹵21.7 nm and the entrapment efficiency is 38.4 鹵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 鹵148,492.40), which was significantly higher than that in the free artesunate group (139 500.00 鹵20 506.10) and Art-PLGA group (163 500.00 鹵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.
【作者單位】： Department
【分類號】：R943;R965

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