载姜黄素纳米结构脂质载体的体内抗疟活性。
In vivo Antiplasmodial Activity of Curcumin-Loaded Nanostructured Lipid Carriers.
机构信息
Cancer Gene Therapy Research Center, Zanjan University of Medical Sciences, Zanjan, Iran.
Department of Pharmaceutical Biomaterials, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
出版信息
Curr Drug Deliv. 2019;16(10):923-930. doi: 10.2174/1567201816666191029121036.
BACKGROUND
It has been shown that curcumin (Cur) has anti-plasmodial activity; however, its weak bioavailability, rapid metabolism, and limited chemical stability have restricted its application in clinical usages. Nanostructured lipid carriers (NLCs) are a type of Drug-Delivery Systems (DDSs) whose core matrix is composed of both solid and liquid lipids.
OBJECTIVE
The aim of the current study was to prepare and characterize curcumin-loaded nanostructured lipid carriers (Cur-NLC) for malaria treatment.
METHODS
For producing NLC, coconut oil and cetyl palmitate were selected as a liquid and solid lipid, respectively. In order to prepare the Cur-NLC, the microemulsion method was applied. General toxicity assay on Artemia salina as well as hemocompatibility was investigated. Anti-plasmodial activity was studied on mice infected with Plasmodium berghei.
RESULTS
The NLCs mean particle size and Polydispersity Index (PI) were 145 nm and 0.3, respectively. Further, the zeta potential of the Cur-NLC was -25 mV. The NLCs indicated a pseudo-spherical shape observed via transmission electron microscopy (TEM). The loading capacity and encapsulation efficacy of the obtained Cur-NLC were 3.1 ± 0.015% and 74 ± 3.32%, respectively. In vitro, Cur release profiles showed a sustained-release pattern up to 5 days in the synthesized Cur-NLC. The results of in vivo antiplasmodial activity against P. berghei revealed that antimalarial activity of Cur-NLC was significantly higher compared with that of free Cur at the dose of 40 mg/kg/day.
CONCLUSION
The results of this study suggested that NLC would be used as a potential nanocarrier for the treatment of malaria.
背景
姜黄素（Cur）具有抗疟原虫活性；然而，其生物利用度低、代谢快、化学稳定性有限，限制了其在临床应用中的应用。纳米结构脂质载体（NLC）是一种药物传递系统（DDS），其核心基质由固体和液体脂质组成。
目的
本研究旨在制备和表征用于疟疾治疗的载姜黄素纳米结构脂质载体（Cur-NLC）。
方法
为了制备 NLC，选择椰子油和十六烷醇棕榈酸酯分别作为液体和固体脂质。为了制备 Cur-NLC，应用了微乳液法。研究了对卤虫的一般毒性试验和血液相容性。研究了对感染伯氏疟原虫的小鼠的抗疟原虫活性。
结果
NLC 的平均粒径和多分散指数（PI）分别为 145nm 和 0.3。此外，Cur-NLC 的zeta 电位为-25mV。通过透射电子显微镜（TEM）观察到 NLC 呈伪球形。所获得的 Cur-NLC 的载药量和包封效率分别为 3.1±0.015%和 74±3.32%。体外，Cur 释放曲线显示在合成的 Cur-NLC 中可达到 5 天的持续释放模式。体内抗伯氏疟原虫活性的结果表明，Cur-NLC 的抗疟活性在 40mg/kg/天的剂量下明显高于游离 Cur。
结论
本研究结果表明，NLC 可作为治疗疟疾的潜在纳米载体。
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