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

Qihong Zhang, Nikolay E. Polyakov, Yulia S. Chistyachenko, Mikhail V. Khvostov, Tatjana S. Frolova, Tatjana G. Tolstikova, Alexandr V. Dushkin, Weike Su

Research output: Contribution to journalArticlepeer-review

38 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)198-209
Number of pages12
JournalDrug Delivery
Volume25
Issue number1
DOIs
Publication statusPublished - 5 Jan 2018

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

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