Enhanced Dissolution and Bioavailability of Curcumin Nanocrystals Prepared by Hot Melt Extrusion Technology.
| Autor: | Zhao Y; College of Pharmacy, Zhejiang University of Technology, Hangzhou, People's Republic of China., Xu X; College of Pharmacy, Zhejiang University of Technology, Hangzhou, People's Republic of China., Dai A; Department of Pharmacy, The 903rd Hospital of People's Liberation Army, Hangzhou, People's Republic of China., Jia Y; College of Pharmacy, Zhejiang University of Technology, Hangzhou, People's Republic of China., Wang W; College of Pharmacy, Zhejiang University of Technology, Hangzhou, People's Republic of China. |
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| Jazyk: | angličtina |
| Zdroj: | International journal of nanomedicine [Int J Nanomedicine] 2024 Jun 12; Vol. 19, pp. 5721-5737. Date of Electronic Publication: 2024 Jun 12 (Print Publication: 2024). |
| DOI: | 10.2147/IJN.S463918 |
| Abstrakt: | Purpose: Curcumin nanocrystals (Cur-NCs) were prepared by hot melt extrusion (HME) technology to improve the dissolution and bioavailability of curcumin (Cur). Methods: Cur-NCs with different drug-carrier ratios were prepared by one-step extrusion process with Eudragit ® EPO (EEP) as the carrier. The dispersed size and solid state of Cur in extruded samples were characterized by dynamic light scattering (DLS), scanning electron microscope (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). The thermal stability of Cur was analyzed by thermogravimetric analysis (TGA) and high performance liquid chromatography (HPLC). Dissolution and pharmacokinetics were studied to evaluate the improvement of dissolution and absorption of Cur by nano-preparation. Results: Cur-NCs with particle sizes in the range of 50~150 nm were successfully prepared by using drug-carrier ratios of 1:1, 2:1 and 4:1, and the crystal form of Cur was Form 1 both before and after HME. The extrudate powders showed very efficient dissolution with the cumulative dissolution percentage of 80% in less than 2 min, and the intrinsic dissolution rates of them were 13.68 ± 1.20 mg/min/cm 2 , 11.78 ± 0.57 mg/min/cm 2 and 4.35 ± 0.20 mg/min/cm 2 , respectively, whereas that of pure Cur was only 0.04 ± 0.00 mg/min/cm 2 . The TGA data demonstrated that the degradation temperature of Cur was about 250 °C, while the HPLC results showed Cur was degraded when extruded at the temperature over 150 °C. Pharmacokinetic experiment showed a significant improvement in the absorption of Cur. The C Conclusion: Cur-NCs can be prepared by HME technology in one step, which significantly improves the dissolution and bioavailability of Cur. Such a novel method for preparing insoluble drug nanocrystals has broad application prospects. Competing Interests: The authors report no conflicts of interest in this work. (© 2024 Zhao et al.) |
| Databáze: | MEDLINE |
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