Preparation and characterization of soluble branched ionic β-cyclodextrins and their inclusion complexes with triclosan

Carbohydr Polym. 2016 May 20:142:149-57. doi: 10.1016/j.carbpol.2016.01.046. Epub 2016 Jan 23.

Abstract

This study aims to synthesize, characterize and investigate the water solubility and cytotoxicity of branched anionic/cationic β-cyclodextrins (bβCDs) obtained by reaction with epichlorohydrin and chloroacetic acid or choline chloride, respectively, by a single step polycondensation reaction. Obtained ionic bβCDs were investigated as an attempt to comparatively study anionic and cationic bβCDs. Water solubility of both ionic derivatives was similar (400 mg/mL) at neutral and basic pHs and remarkably higher than that of their neutral homologues. Additionally, a pH-dependent solubility of anionic bβCDs was observed. Cytotoxicity of ionic bβCDs was evaluated on Human colon carcinoma Caco-2 cells and high cell viability (>99%) was observed in the range of 0-100 mg/mL for anionic and cationic samples, in the same range of that of neutral and parent β-CDs. Additionally, complexes formation capacity with triclosan, a poor water soluble antimicrobial agent, was confirmed by several techniques observing a complexation limit around 4 mg/mL for both systems and higher stability constant for anionic bβCDs than cationic derivatives.

Keywords: Branched ionic cyclodextrins; Cytotoxicity; Epichlorohydrin; Water solubility.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetates / chemical synthesis
  • Acetates / chemistry
  • Anti-Infective Agents, Local / administration & dosage*
  • Anti-Infective Agents, Local / chemistry
  • Caco-2 Cells
  • Cell Survival / drug effects
  • Drug Carriers / adverse effects
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry*
  • Epichlorohydrin / chemical synthesis
  • Epichlorohydrin / chemistry
  • Humans
  • Ions / adverse effects
  • Ions / chemical synthesis
  • Ions / chemistry
  • Solubility
  • Triclosan / administration & dosage*
  • Triclosan / chemistry
  • Water / chemistry
  • beta-Cyclodextrins / adverse effects
  • beta-Cyclodextrins / chemical synthesis
  • beta-Cyclodextrins / chemistry*

Substances

  • Acetates
  • Anti-Infective Agents, Local
  • Drug Carriers
  • Ions
  • beta-Cyclodextrins
  • Water
  • Epichlorohydrin
  • Triclosan
  • chloroacetic acid