Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry

Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry Full article

Journal

Drug Delivery
ISSN: 1071-7544 , E-ISSN: 1521-0464

Output data

Year: 2018, Volume: 25, Number: 1, Pages: 198-209 Pages count : 12 DOI: 10.1080/10717544.2017.1422298

Tags

Bioavailability; Curcumin; Cytotoxic activity; Mechanical ball milling; Self-micelle; Solid dispersion

Authors

Zhang Qihong ¹ , Polyakov Nikolay E. ² , Chistyachenko Yulia S. ³ , Khvostov Mikhail V. ^4,5 , Frolova Tatjana S. ^4,5,6 , Tolstikova Tatjana G. ^4,5 , Dushkin Alexandr V. ³ , Su Weike ^1,7

Affiliations

1	(Scopus) National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou, China
2	(Scopus) Institute of Chemical Kinetics and Combustion, Novosibirsk, Russian Federation
3	(Scopus) Institute of Solid State Chemistry and Mechanochemistry, Novosibirsk, Russian Federation
4	(Scopus) N.N. Vorozhtsov Institute of Organic Chemistry SB RAS, Novosibirsk, Russian Federation
5	(Scopus) Novosibirsk State University, Novosibirsk, Russian Federation
6	(Scopus) Institute of Cytology and Genetics SB RAS, Novosibirsk, Russian Federation
7	(Scopus) Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, China

An amorphous solid dispersion (SD) of curcumin (Cur) with disodium glycyrrhizin (Na2GA) was prepared by mechanical ball milling. Curcumin loaded micelles were self-formed by Na2GA when SD dissolved in water. The physical properties of Cur SD in solid state were characterized by differential scanning calorimetry, X-ray diffraction studies, and scanning electron microscope. The characteristics of the sample solutions were analyzed by reverse phase HPLC, UV–visible spectroscopy, 1H NMR spectroscopy, gel permeation LC, and transmission electron microscopy. In vitro cytotoxic tests demonstrated that Cur SD induced higher cytotoxicity against glioblastoma U-87MG cells than free Cur. Besides, an improvement of membrane permeability of Cur SD was confirmed by parallel artificial membrane permeability assay. Further pharmacokinetic study of this SD formulation in rat showed a significant ~19- fold increase of bioavailability as comparing to free Cur. Thus, Cur SD provide a more potent and efficacious formulation for Cur oral delivery. © 2017 The Author(s).

Zhang Q. , Polyakov N.E. , Chistyachenko Y.S. , Khvostov M.V. , Frolova T.S. , Tolstikova T.G. , Dushkin A.V. , Su W.
Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry

Drug Delivery. 2018. V.25. N1. P.198-209. DOI: 10.1080/10717544.2017.1422298 WOS Scopus РИНЦ

Full text from publisher

Published print:	Jan 1, 2018
Published online:	Jan 5, 2018

Web of science	WOS:000426911800002
Scopus	2-s2.0-85048706581
Elibrary	35717698
OpenAlex	W2782161826