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具有溶解度增强作用的姜黄素纳米混悬液的制备及体外/体内评价

Preparation and in-vitro/in-vivo evaluation of curcumin nanosuspension with solubility enhancement.

作者信息

Li Xin, Yuan Huiling, Zhang Caiyun, Chen Weidong, Cheng Weiye, Chen Xin, Ye Xi

机构信息

College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, China.

出版信息

J Pharm Pharmacol. 2016 Aug;68(8):980-8. doi: 10.1111/jphp.12575. Epub 2016 Jun 10.


DOI:10.1111/jphp.12575
PMID:27283220
Abstract

OBJECTIVES: We developed Cur nanosuspension (Cur-NS) with PVPK30 and SDS as stabilizers to improve poor water solubility and short biological half-time of Cur. METHODS: Physicochemical characterization of Cur-NS was characterized systematically. The in-vitro dissolution, cytotoxicity and in-vivo pharmacokinetic experiments of Cur-NS were also evaluated. KEY FINDINGS: Scanning electron microscope indicated that the morphologies of Cur-NS were spherical or ellipsoidal in shape. X-ray diffraction verified that Cur was successfully developed as nanoparticles with an amorphous phase in Cur-NS. Fourier transform infrared spectroscopy suggested there was no degradation about Cur in the Cur-NS. Furthermore, the in-vitro study showed that the cumulative release of the Cur-NS was 82.16 ± 2.62% within 34 h and the cytotoxicity of the Cur-NS against HepG2 cells was much better than raw Cur. Besides, in-vivo pharmacokinetics in rats by intravenous injection displayed that the in-vivo process of Cur-NS pertained to two-compartment model. Meanwhile, the t1/2 and AUC0-t of Cur-NS were enhanced by 11.0-fold and 4.2-fold comparing to Cur solution. CONCLUSIONS: The Cur-NS significantly increased the water solubility and half-time of Cur, suggesting its potential as a nanocarrier in the delivery of Cur for future clinical application.

摘要

目的:我们以聚乙烯吡咯烷酮K30(PVPK30)和十二烷基硫酸钠(SDS)作为稳定剂开发了姜黄素纳米混悬液(Cur-NS),以改善姜黄素水溶性差和生物半衰期短的问题。 方法:系统地表征了Cur-NS的理化性质。还评估了Cur-NS的体外溶出度、细胞毒性和体内药代动力学实验。 主要发现:扫描电子显微镜表明Cur-NS的形态为球形或椭圆形。X射线衍射证实Cur在Cur-NS中成功开发为具有非晶相的纳米颗粒。傅里叶变换红外光谱表明Cur-NS中的Cur没有降解。此外,体外研究表明,Cur-NS在34小时内的累积释放率为82.16±2.62%,Cur-NS对HepG2细胞的细胞毒性比原料药姜黄素要好得多。此外,大鼠静脉注射的体内药代动力学显示,Cur-NS的体内过程符合二室模型。同时,与姜黄素溶液相比,Cur-NS的t1/2和AUC0-t分别提高了11.0倍和4.2倍。 结论:Cur-NS显著提高了姜黄素的水溶性和半衰期,表明其作为姜黄素递送的纳米载体在未来临床应用中的潜力。

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Preparation and in-vitro/in-vivo evaluation of curcumin nanosuspension with solubility enhancement.

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