Статья

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

Qihong ZhangNational 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, PR China;Nikolay E. PolyakovInstitute of Chemical Kinetics and Combustion, Novosibirsk, Russia;Yulia S. ChistyachenkoInstitute of Solid State Chemistry and Mechanochemistry, Novosibirsk, Russia;Михаил В. ХвостовN.N. Vorozhtsov Institute of Organic Chemistry SB RAS, Novosibirsk, Russia;Tatjana S. FrolovaInstitute of Cytology and Genetics SB RAS, Novosibirsk, Russia;Т. Г. ТолстиковаNovosibirsk State University, Novosibirsk, Russia;Alexander V. DushkinInstitute of Solid State Chemistry and Mechanochemistry, Novosibirsk, Russia;Weike SuKey Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, PR China

2018en

ABI

Аннотация

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-87 MG 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.

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Идентификаторы

DOI: 10.1080/10717544.2017.1422298

Цитирования и источники

Цитирований: 2Использованных источников: 0

Показатели — AkademScholar