Cationic cyclodextrin/alginate chitosan nanoflowers as 5-fluorouracil drug delivery system

Mater Sci Eng C Mater Biol Appl. 2017 Jan 1;70(Pt 1):169-177. doi: 10.1016/j.msec.2016.08.073. Epub 2016 Aug 29.

Abstract

Cyclodextrins (CDs) have widely been used as component of drug delivery systems. However unmodified cyclodextrins are associated with cytotoxicity and poor water solubility thus limiting their use in pharmaceutical industry. The cationic-β-cyclodextrin (Cat-β-CD) polymer cores were synthesized using β-CD, epichlorohydrin and choline chloride via a one-step polycondensation process. The main aim of this study was to synthesize hierarchical nanoflowers composed of cationic-β-CD as polymeric core along with alginate and chitosan "petals" (Cat-β-CD/Alg-Chi nanoflowers) as carriers for oral delivery of 5-Fluorouracil (5-FU) via an ionic-gelation technique. The drug loading capacity, particle size, zeta potential and surface morphology of the synthesized nanoflowers were determined. The prepared nanoflowers were formed with an average size of 300nm and a zeta potential of +9.90mV with good encapsulation efficiency of up to 77.3%. In vitro release of 5-FU from the loaded nanoflowers showed controlled and sustained release compared to the inclusion complex alone. Cat-β-CD/Alg-Chi nanoflowers were assessed against L929 cells and found to be effectively inhibiting the growth of L929 cells in a concentration dependent manner.

Keywords: 5-Fluorouracil; Alginate; Cationic-β-cyclodextrin; Chitosan; Inclusion complex and oral delivery system; Nanoflowers.

MeSH terms

  • Alginates / chemistry*
  • Animals
  • Calorimetry, Differential Scanning
  • Cations
  • Cell Death / drug effects
  • Chitosan / chemistry*
  • Drug Delivery Systems / methods*
  • Drug Liberation
  • Fibroblasts / cytology
  • Fibroblasts / drug effects
  • Fluorouracil / pharmacology*
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Mice
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size
  • Proton Magnetic Resonance Spectroscopy
  • Spectroscopy, Fourier Transform Infrared
  • Static Electricity
  • beta-Cyclodextrins

Substances

  • Alginates
  • Cations
  • Hexuronic Acids
  • beta-Cyclodextrins
  • Glucuronic Acid
  • Chitosan
  • betadex
  • Fluorouracil