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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.

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Zhang Q, Polyakov NE, Chistyachenko YS, Khvostov MV, Frolova TS, Tolstikova TG et al. Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry. Drug Delivery. 2018 Jan 5;25(1):198-209. doi: 10.1080/10717544.2017.1422298

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Zhang, Qihong ; Polyakov, Nikolay E. ; Chistyachenko, Yulia S. et al. / Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry. In: Drug Delivery. 2018 ; Vol. 25, No. 1. pp. 198-209.

BibTeX

@article{14c344f3d15a410d8380c208f26aca5b,
title = "Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry",
abstract = "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.",
keywords = "Bioavailability, Curcumin, Cytotoxic activity, Mechanical ball milling, Self-micelle, Solid dispersion, Glycyrrhizic Acid/chemistry, Humans, Biological Availability, Male, Calorimetry, Differential Scanning/methods, Drug Carriers/chemistry, MCF-7 Cells, Micelles, X-Ray Diffraction/methods, Rats, Permeability, Water/chemistry, Rats, Sprague-Dawley, Particle Size, Glioblastoma/drug therapy, Animals, Cell Line, Tumor, Chemistry, Pharmaceutical/methods, Curcumin/chemistry, ANGIOGENESIS, PROLIFERATION, CARRIER, DELIVERY, GLYCYRRHIZIC ACID, self-micelle, ORAL BIOAVAILABILITY, PERSPECTIVES, cytotoxic activity, curcumin, VITRO, FORMULATION, bioavailability, solid dispersion, IN-VIVO",
author = "Qihong Zhang and Polyakov, {Nikolay E.} and Chistyachenko, {Yulia S.} and Khvostov, {Mikhail V.} and Frolova, {Tatjana S.} and Tolstikova, {Tatjana G.} and Dushkin, {Alexandr V.} and Weike Su",
note = "Publisher Copyright: {\textcopyright} 2017 The Author(s).",
year = "2018",
month = jan,
day = "5",
doi = "10.1080/10717544.2017.1422298",
language = "English",
volume = "25",
pages = "198--209",
journal = "Drug Delivery",
issn = "1071-7544",
publisher = "Informa Healthcare",
number = "1",

}

RIS

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