Preparation and in-vitro/in-vivo evaluation of curcumin nanosuspension with solubility enhancement. (10th June 2016)

• Record Type: Journal Article
• Authors: Li, Xin; Yuan, Huiling; Zhang, Caiyun; Chen, Weidong; Cheng, Weiye; Chen, Xin; Ye, Xi
• Is Part Of: Journal of pharmacy and pharmacology. Volume 68:Number 8(2016:Aug.)
• Page Start: 980
• Page End: 988
• Publication Date: 2016-06-10
• Subjects: curcumin -- cytotoxicity -- intravenous injection -- nanosuspension -- pharmacokinetics; Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.12575
• Languages: English
• ISSNs: 0022-3573

Abstract

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 t 1/2 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.