Nano-precipitated curcumin loaded particles: effect of carrier size and drug complexation with (2-hydroxypropyl)-β-cyclodextrin on their biological performances

Int J Pharm. 2017 Mar 30;520(1-2):21-28. doi: 10.1016/j.ijpharm.2017.01.049. Epub 2017 Jan 24.

Abstract

In this work, curcumin (CURC)-encapsulating nanoparticles (NPs), made up of an amphiphilic blend of poloxamers and PLGA (PPC NPs) at different polymer concentrations, were prepared by nanoprecipitation. CURC was preliminarily complexed with (2-hydroxypropyl)-β-cyclodextrin (HPβCD) to improve its loading efficiency. The formation of host-guest complexes of CURC with HPβCD (CD-CURC) was confirmed by means of 1HNMR studies and differential scanning calorimetry (DSC). Nanoprecipitation allowed to obtain NPs with a small size (90-120nm depending on the polymer concentration), a narrow size distribution and stable in water for 30days at 4°C and in RPMI-1640 cell culture medium up to 72h at 37°C. The in vitro release of CD-CURC, sustained up to 5days, was governed mainly by a diffusive mechanism. It was also found that the produced NPs were efficiently internalized by mesothelioma cells (MSTO-211H) in the cytoplasmic space, at an extent strongly dependent on NP size and polydispesity index, therefore pointing at the importance of NP preparation method in improving their uptake.

Keywords: Curcumin; Cyclodextrin; Mesothelioma; Nanoparticles; PLGA; Poloxamers.

MeSH terms

  • 2-Hydroxypropyl-beta-cyclodextrin
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cells, Cultured
  • Chemical Precipitation
  • Curcumin / administration & dosage
  • Curcumin / chemistry*
  • Curcumin / pharmacokinetics
  • Curcumin / pharmacology*
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Drug Stability
  • Humans
  • Lactic Acid / chemistry
  • Nanoparticles / chemistry*
  • Nanoparticles / metabolism
  • Particle Size
  • Poloxamer / chemistry
  • Polyglycolic Acid / chemistry
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • beta-Cyclodextrins / chemistry*

Substances

  • Drug Carriers
  • beta-Cyclodextrins
  • Poloxamer
  • 2-Hydroxypropyl-beta-cyclodextrin
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Curcumin