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Stabilizing effect of the cyclodextrins additive to spray-dried particles of curcumin/polyvinylpyrrolidone on the supersaturated state of curcumin
Authors:Satoshi Nogami  Katsuhiko Minoura  Nao Kiminami  Yui Kitaura  Hiromasa Uchiyama  Kazunori Kadota  Yuichi Tozuka
Affiliation:Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan
Abstract:Although curcumin is considered to have various therapeutic effects, its use as a functional food or supplement is restricted owing to its low water solubility and bioavailability. To increase the solubility of curcumin in water, the use of polyvinylpyrrolidone (PVP) and vinylpyrrolidone-vinyl acetate copolymers with a pyrrolidone skeleton was noted to be promising. In particular, the bi-component formulations of curcumin/PVP prepared through spray drying exhibited an amorphous state in powder X-ray diffraction observations and temporally increased the apparent solubility of curcumin to over 5000 times that of untreated curcumin; nevertheless, after 24 h, the solubility decreased owing to the unstable supersaturated state of curcumin. The addition of α-cyclodextrin (α-CyD) in the bi-component curcumin/PVP formulation helped maintain the supersaturated state of curcumin, whereas the addition of β- and γ-CyD led to the collapse of the supersaturated state. The addition of α-CyD can likely help inhibit the nucleation and crystal growth of curcumin, through the interaction among the solubilized units of curcumin/PVP and α-CyD.
Keywords:Amorphous solid dispersion  FTIR  Pyrrolidone skeleton  Spray drying  Supersaturation  CyD"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0035"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  cyclodextrin  FTIR"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0045"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  Fourier transfer infrared spectroscopy  HPC"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0055"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  hydroxypropyl cellulose  HPMC"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0065"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  hydroxypropyl methylcellulose  PM"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0075"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  physical mixture  PVA"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0085"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  polyvinyl alcohol  PVP"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0095"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  polyvinylpyrrolidone  PXRD"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0105"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  powder X-ray diffraction  VA"  },{"  #name"  :"  keyword"  ,"  $"  :{"  id"  :"  k0115"  },"  $$"  :[{"  #name"  :"  text"  ,"  _"  :"  vinylpyrrolidone-vinyl acetate copolymer
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