穿心莲内酯-羧甲基壳聚糖纳米粒的研制：表征、释放及抗疟活性研究
Development of Andrographolide-Carboxymethyl Chitosan Nanoparticles: Characterization, Release and Antimalarial Activity Study.
作者信息
Sari Retno, Widyawaruyanti Aty, Anindita Franciscus B Tedy, Astuti Sinta Kusuma, Setyawan Dwi
机构信息
Airlangga University, Faculty of Pharmacy, Department of Pharmaceutics, Surabaya, Indonesia.
Airlangga University, Faculty of Pharmacy, Department of Pharmacognosy and Phytochemistry, Surabaya, Indonesia.
出版信息
Turk J Pharm Sci. 2018 Aug;15(2):136-141. doi: 10.4274/tjps.53825. Epub 2018 Jul 17.
OBJECTIVES
The purpose of this study was to investigate the effect of andrographolide-carboxymethyl chitosan nanoparticles formation on the physical characteristics, release profile and antimalarial activity of andrographolide.
MATERIALS AND METHODS
Nanoparticles were prepared by ionic gelation method-spray drying using CaCl as the crosslinker with a composition of drug: polymer: CaCl=40: 250: 100. The obtained particles were evaluated for its size and morphology; physical state, drug content, drug release and antimalarial activity on infected mice.
RESULTS
The results of DTA and XRD showed that nanoparticle systems had a lower melting point and lower crystallinity degree. The drug dissolved from the nanoparticles was increased up to 6.5 times and the antimalarial activity was 1.65 times higher compared to andrographolide.
CONCLUSION
The formation andrographolide-carboxymethyl chitosan nanoparticles affected the physical characte-ristics of andrographolide. The decrease crystallinity of andrographolide resulted in a lower melting point of andrographolide. Such changes provided a positive impact to the drug dissolution and then its activity.
目的
本研究旨在探讨穿心莲内酯-羧甲基壳聚糖纳米粒的形成对穿心莲内酯物理特性、释放曲线及抗疟活性的影响。
材料与方法
采用离子凝胶法-喷雾干燥，以氯化钙作为交联剂，按照药物：聚合物：氯化钙=40: 250: 100的组成制备纳米粒。对所得颗粒的大小和形态、物理状态、药物含量、药物释放及对感染小鼠的抗疟活性进行评估。
结果
差示热分析（DTA）和X射线衍射（XRD）结果表明，纳米粒体系具有较低的熔点和结晶度。与穿心莲内酯相比，纳米粒中药物的溶出量增加了6.5倍，抗疟活性提高了1.65倍。
结论
穿心莲内酯-羧甲基壳聚糖纳米粒的形成影响了穿心莲内酯的物理特性。穿心莲内酯结晶度的降低导致其熔点降低。这些变化对药物溶出进而对其活性产生了积极影响。
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