Preparation, physicochemical and pharmacological study of curcumin solid dispersion with an arabinogalactan complexation agent

Preparation, physicochemical and pharmacological study of curcumin solid dispersion with an arabinogalactan complexation agent Full article

Journal

International Journal of Biological Macromolecules
ISSN: 0141-8130 , E-ISSN: 1879-0003

Output data

Year: 2019, Volume: 128, Pages: 158-166 Pages count : 9 DOI: 10.1016/j.ijbiomac.2019.01.079

Authors

Zhang Qihong ¹ , Suntsova Lubov ³ , Chistyachenko Yulia S. ³ , Evseenko Veronika ³ , Khvostov Mikhail V. ^4,6 , Polyakov Nikolay E. ⁵ , Dushkin Alexandr V. ^1,3 , Su Weike ^1,2

Affiliations

1	(Данные Web of science) Zhejiang Univ Technol, Collaborat Innovat Ctr Yangtze River Delta Reg Gr, Natl Engn Res Ctr Proc Dev Act Pharmaceut Ingredi, Hangzhou 310014, Zhejiang, Peoples R China
2	(Данные Web of science) Zhejiang Univ Technol, Coll Pharmaceut Sci, Minist Educ, Key Lab Green Pharmaceut Technol & Related Equipm, Hangzhou 310014, Zhejiang, Peoples R China
3	(Данные Web of science) Inst Solid State Chem & Mechanochem, Novosibirsk, Russia
4	(Данные Web of science) Inst Organ Chem, Novosibirsk, Russia
5	(Данные Web of science) Inst Chem Kinet & Combust, Novosibirsk, Russia
6	(Данные Web of science) Inst Cytol & Genet SB RAS, Novosibirsk, Russia

Pharmaceutical solid dispersions (SD) of curcumin (Cur) with macromolecule polysaccharide arabinogalactan (AG) from wood of Larix sibirica were prepared by mechanical ball milling. The physical properties of the dispersed curcumin mixture in solid state were characterized by scanning electron microscope, differential scanning calorimetry and powder X-ray diffraction studies. These methods showed a strong decrease in the degree of crystallinity of Cur and its transformation to amorphization state, accompanied by the formation of the guest-host type complexes. The behavior of the samples in solutions was characterized by reverse phase HPLC, H-1 NMR spectroscopy, UV-Visible spectroscopy and gel permeation chromatography (GPC). Mechanochemically prepared complexes demonstrated the increased solubility of Cur up to similar to 10.5 times in contrast to pure curcumin. The rapid storage test showed high chemical stability of Cur, which depended on mass relations of Cur-AG. Besides, improved membrane permeability of Cur-AG SD was tested by parallel artificial membrane permeability assay. Pharmacokinetic study of Cur-AG SD formulation in rat demonstrated a significant similar to 8-fold enhancement of bioavailability in comparison to pure curcumin. In MTT tests, Cur-AG SD showed moderate cytotoxicity against human glioblastoma cells and immortalized human fibroblasts. Therefore, Cur-AG solid dispersion was a more promising and efficacious formulation for application in oral drug delivery. (C) 2019 Elsevier B.V. All rights reserved.

Zhang Q. , Suntsova L. , Chistyachenko Y.S. , Evseenko V. , Khvostov M.V. , Polyakov N.E. , Dushkin A.V. , Su W.
Preparation, physicochemical and pharmacological study of curcumin solid dispersion with an arabinogalactan complexation agent
International Journal of Biological Macromolecules. 2019. V.128. P.158-166. DOI: 10.1016/j.ijbiomac.2019.01.079 WOS Scopus

Published print:

May 1, 2019

Web of science	WOS:000463305100021
Scopus	2-s2.0-85060485249
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