Improved curcumin loading, release, solubility and toxicity by tuning the molar ratio of cross-linker to β-cyclodextrin

Carbohydr Polym. 2019 Jun 1:213:70-78. doi: 10.1016/j.carbpol.2019.02.075. Epub 2019 Feb 22.

Abstract

A novel β-cyclodextrin-based nanosponge (CDNS) was proposed as curcumin (CUR) delivery system improving pharmacokinetics and anticancer activity of CUR. The effect of molar ratio of Epiclon (EPI) as cross-linker and β-cyclodextrin (βCD) on the porosity, surface area, swelling ratio, CUR solubility and loading capacity, rate of drug release and selective toxicity of the CDNSs was fully investigated. The high degree of cross-linking led to the formation of mesoporous CDNS having high specific surface area and high loading capacity. All CUR-free CDNSs showed no toxicity against MCF 10A and 4T1 cells as normal and cancerous cells, respectively. While CDNSs-CUR exhibited selective toxicity against cancerous cells. In sum, high CUR aqueous solubility, significant loading and controllable release of the CUR, outstanding and selective toxicity against cancerous cells make CDNS8-CUR (EPI/βCD = 8) as promising candidate for further study in the cancer therapy.

Keywords: Curcumin; Epiclon; MCF 10A and 4T1 cells; Nanosponge; β-Cyclodextrin.

MeSH terms

  • Animals
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cross-Linking Reagents / administration & dosage
  • Cross-Linking Reagents / chemistry
  • Cross-Linking Reagents / pharmacology*
  • Curcumin / administration & dosage
  • Curcumin / chemistry
  • Curcumin / toxicity*
  • Dose-Response Relationship, Drug
  • Drug Delivery Systems
  • Humans
  • Mice
  • Molecular Structure
  • Nanoparticles / chemistry*
  • Particle Size
  • Solubility
  • Structure-Activity Relationship
  • Surface Properties
  • Thermodynamics
  • beta-Cyclodextrins / chemistry
  • beta-Cyclodextrins / pharmacology*

Substances

  • Cross-Linking Reagents
  • beta-Cyclodextrins
  • Curcumin