دورية أكاديمية

Enhanced Dissolution and Bioavailability of Curcumin Nanocrystals Prepared by Hot Melt Extrusion Technology.

التفاصيل البيبلوغرافية
العنوان: Enhanced Dissolution and Bioavailability of Curcumin Nanocrystals Prepared by Hot Melt Extrusion Technology.
المؤلفون: 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.
المصدر: 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).
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: DOVE Medical Press Country of Publication: New Zealand NLM ID: 101263847 Publication Model: eCollection Cited Medium: Internet ISSN: 1178-2013 (Electronic) Linking ISSN: 11769114 NLM ISO Abbreviation: Int J Nanomedicine Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Auckland : DOVE Medical Press,
مواضيع طبية MeSH: Curcumin*/pharmacokinetics , Curcumin*/chemistry , Curcumin*/administration & dosage , Nanoparticles*/chemistry , Biological Availability* , Particle Size* , Solubility* , Hot Melt Extrusion Technology*/methods, Animals ; Drug Carriers/chemistry ; Drug Carriers/pharmacokinetics ; Male ; Calorimetry, Differential Scanning ; Drug Stability ; Drug Liberation ; X-Ray Diffraction ; Polymethacrylic Acids
مستخلص: 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 max of Cur in the Cur-NC group was 1.68 times that of pure Cur group, and the C max and area under the curve (AUC 0-∞ ) of metabolites were 2.79 and 4.07 times compared with pure Cur group.
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.)
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فهرسة مساهمة: Keywords: absorption in vivo; curcumin; dissolution; hot melt extrusion technology; nanocrystals
المشرفين على المادة: IT942ZTH98 (Curcumin)
0 (Drug Carriers)
905HNO1SIH (Eudragit E PO)
0 (Polymethacrylic Acids)
تواريخ الأحداث: Date Created: 20240619 Date Completed: 20240619 Latest Revision: 20240620
رمز التحديث: 20240620
مُعرف محوري في PubMed: PMC11182756
DOI: 10.2147/IJN.S463918
PMID: 38895153
قاعدة البيانات: MEDLINE
الوصف
تدمد:1178-2013
DOI:10.2147/IJN.S463918