Research output: Contribution to journal › Article › peer-review
Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry. / Zhang, Qihong; Polyakov, Nikolay E.; Chistyachenko, Yulia S. et al.
In: Drug Delivery, Vol. 25, No. 1, 05.01.2018, p. 198-209.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry
AU - Zhang, Qihong
AU - Polyakov, Nikolay E.
AU - Chistyachenko, Yulia S.
AU - Khvostov, Mikhail V.
AU - Frolova, Tatjana S.
AU - Tolstikova, Tatjana G.
AU - Dushkin, Alexandr V.
AU - Su, Weike
N1 - Publisher Copyright: © 2017 The Author(s).
PY - 2018/1/5
Y1 - 2018/1/5
N2 - 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.
AB - 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.
KW - Bioavailability
KW - Curcumin
KW - Cytotoxic activity
KW - Mechanical ball milling
KW - Self-micelle
KW - Solid dispersion
KW - Glycyrrhizic Acid/chemistry
KW - Humans
KW - Biological Availability
KW - Male
KW - Calorimetry, Differential Scanning/methods
KW - Drug Carriers/chemistry
KW - MCF-7 Cells
KW - Micelles
KW - X-Ray Diffraction/methods
KW - Rats
KW - Permeability
KW - Water/chemistry
KW - Rats, Sprague-Dawley
KW - Particle Size
KW - Glioblastoma/drug therapy
KW - Animals
KW - Cell Line, Tumor
KW - Chemistry, Pharmaceutical/methods
KW - Curcumin/chemistry
KW - ANGIOGENESIS
KW - PROLIFERATION
KW - CARRIER
KW - DELIVERY
KW - GLYCYRRHIZIC ACID
KW - self-micelle
KW - ORAL BIOAVAILABILITY
KW - PERSPECTIVES
KW - cytotoxic activity
KW - curcumin
KW - VITRO
KW - FORMULATION
KW - bioavailability
KW - solid dispersion
KW - IN-VIVO
UR - http://www.scopus.com/inward/record.url?scp=85048706581&partnerID=8YFLogxK
U2 - 10.1080/10717544.2017.1422298
DO - 10.1080/10717544.2017.1422298
M3 - Article
C2 - 29302995
AN - SCOPUS:85048706581
VL - 25
SP - 198
EP - 209
JO - Drug Delivery
JF - Drug Delivery
SN - 1071-7544
IS - 1
ER -
ID: 14047873