Background

Malaria is a parasitic lethal disease caused by Plasmodium protozoa. The resistance and drugs’ side effects have led to numerous researches for alternative suitable drugs with better efficiency and lower toxicity

Purpose

In the present study, we investigated in vivo antimalarial effects of G2 linear dendrimer-based nano-chloroquine.

Methods

After the preparation of nano dendrimer G2, chloroquine loading was done. Determine the characterization of particles were specified by DLS, SLS and SEM. The LC–MS and FTIR were used for verifying the nano dendrimer G2 and the loading of chloroquine into the compound. The Solubility N-chloroquine and measurement of drug release rate were done. Antiplasmodial activity of N-chloroquine on BALB/c mice was performed by the microscope and enzymatic methods. At the end, In vivo toxicity of N-chloroquine on tissues was assayed. The RBC morphology and enzyme levels were identified.

Results

The results showed the synthesized N-chloroquine had suitable size and solubility. Highest inhibitory effect on Plasmodium parasitic growth was observed at 16 mg/kg dose of N-chloroquine, which eliminated 95% of the parasites (p > 0.05). ED₅₀ is observed at 7.7 mg/kg of N-chloroquine dose. Biochemical findings showed the synthesized N-chloroquine was safer than chloroquine. The N-chloroquine no adverse effects were observed in examined tissues.

Conclusion

Due to the better effect of the synthesized N-chloroquine on Plasmodium berghei in mice compared to chloroquine, this nanoparticle can be considered as an effective anti-plasmodium compound while more comprehensive research is recommended.

中文翻译：

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负载氯喹的纳米树枝状大分子 G2 对伯氏疟原虫感染小鼠的抗疟原虫作用

背景

疟疾是由疟原虫引起的一种寄生性致死性疾病。耐药性和药物的副作用导致了许多研究以寻找效率更高、毒性更低的替代合适药物

目的

在本研究中，我们研究了基于 G2 线性树枝状大分子的纳米氯喹的体内抗疟作用。

方法

纳米树枝状大分子G2制备完成后，进行氯喹负载。通过 DLS、SLS 和 SEM 确定颗粒的表征。LC-MS 和 FTIR 用于验证纳米树枝状大分子 G2 和氯喹负载到化合物中。进行了溶解度N-氯喹和药物释放速率的测量。N-氯喹对BALB/c小鼠的抗疟原虫活性通过显微镜和酶法进行。最后，测定了N-氯喹对组织的体内毒性。鉴定了红细胞形态和酶水平。

结果

结果表明合成的N-氯喹具有合适的尺寸和溶解度。16 mg/kg剂量的N-氯喹对疟原虫寄生生长的抑制效果最高，可消灭95%的疟原虫( p  > 0.05)。在 7.7 mg/kg N-氯喹剂量下观察到ED _{50 。}生化结果表明合成的N-氯喹比氯喹更安全。在检查的组织中未观察到N-氯喹的副作用。

结论

由于与氯喹相比，合成的N-氯喹对小鼠伯氏疟原虫的作用更好，这种纳米颗粒可以被认为是一种有效的抗疟原虫化合物，同时建议进行更全面的研究。