张强, 叶国庆, 李晔, 杨青松. 环孢素A硬脂酸纳米球的实验研究J. 药学学报, 1999, 34(4): 308-312.
引用本文: 张强, 叶国庆, 李晔, 杨青松. 环孢素A硬脂酸纳米球的实验研究J. 药学学报, 1999, 34(4): 308-312.
Zhang Qiang, Yie Guoqing, Li Yie , Yang Qingsong, . STUDIES ON THE CYCLOSPORIN A LOADED STEARIC ACID NANOPARTICLESJ. Acta Pharmaceutica Sinica, 1999, 34(4): 308-312.
Citation: Zhang Qiang, Yie Guoqing, Li Yie , Yang Qingsong, . STUDIES ON THE CYCLOSPORIN A LOADED STEARIC ACID NANOPARTICLESJ. Acta Pharmaceutica Sinica, 1999, 34(4): 308-312.

环孢素A硬脂酸纳米球的实验研究

STUDIES ON THE CYCLOSPORIN A LOADED STEARIC ACID NANOPARTICLES

  • 摘要: 目的:探讨硬脂酸纳米球作为新型药物载体的可能性。方法:制备了硬脂酸纳米球(SA-NP),用电镜考察其形态,测定了各种理化特性;以环孢素A(CYA)为模型药物,制备了环孢素A硬脂酸纳米球(CYA-SA-NP);对其进行了红外光谱测定和差示扫描量热分析;建立了测定CYA-SA-NP和血中CYA的HPLC法。以市售CYA微乳型口服液为对照,测定了口服CYA-SA-NP在大鼠体内的药代动力学参数和相对生物利用度。结果:CYA-SA-NP的平均粒径为316.6nm,CYA的平均包封率为88.39%,CYA和硬脂酸之间无化学反应发生;CYA-SA-NP的相对生物利用度接近80%,而且达峰时间较晚,具有明显的缓释效果。结论:硬脂酸纳米球将可能成为一种新型的药物载体。

     

    Abstract: AIM: To investigate the possibility of SA-NP (stearic acid nanoparticles) as a new kind of drug carrier. METHODS: SA-NP was prepared by melt-homogenization. Some of its physicochemical properties were investigated. Its morphology was examined by transmission electron microscope. Cyclosporin A (CyA), as a model drug was then encapsulated into SA-NP (CyA-SA-NP). Following the establishment of HPLC method for CyA in CyA-SA-NP or blood samples, the encapsulation ratio of CyA to SA-NP was estimated, and pharmacokinetics as well as bioavailability of CyA-SA-NP after po administration to Wistar rats were studied, using Sandimmun Neoral (an available microemulsion system of CyA) as a control. RESULTS: The mean diameter of CyA-SA-NP was 316.1 nm, while the encapsulation ratio of CyA to SA-NP reached to 88.36%. It was demonstrated by IR spectra and differential scanning calorimetry that no chemical reaction occurred between the CyA and SA. The relative bioavailability of CyA-SA-NP over control was nearly 80%, and the time to reach maximum concentration (Tmax) of CYA after po administration of CYA-SA-NP was significantly delayed than the control, suggesting an obvious sustained release effect. CONCLUSION: SA-NP might be a very potential drug carrier.

     

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