Hemocompatibility of poly(ɛ-caprolactone) lipid-core nanocapsules stabilized with polysorbate 80-lecithin and uncoated or coated with chitosan

Int J Pharm. 2012 Apr 15;426(1-2):271-279. doi: 10.1016/j.ijpharm.2012.01.051. Epub 2012 Feb 1.

Abstract

The hemocompatibility of nanoparticles is of critical importance for their systemic administration as drug delivery systems. Formulations of lipid-core nanocapsules, stabilized with polysorbate 80-lecithin and uncoated or coated with chitosan (LNC and LNC-CS), were prepared and characterized by laser diffraction (D[4,3]: 129 and 134 nm), dynamic light scattering (119 nm and 133 nm), nanoparticle tracking (D50: 124 and 139 nm) and particle mobility (zeta potential: -15.1 mV and +9.3 mV) analysis. In vitro hemocompatibility studies were carried out with mixtures of nanocapsule suspensions in human blood at 2% and 10% (v/v). The prothrombin time showed no significant change independently of the nanocapsule surface potential or its concentration in plasma. Regarding the activated partial thromboplastin time, both suspensions at 2% (v/v) in plasma did not influence the clotting time. Even though suspensions at 10% (v/v) in plasma decreased the clotting times (p<0.05), the values were within the normal range. The ability of plasma to activate the coagulation system was maintained after the addition of the formulations. Suspensions at 2% (v/v) in blood showed no significant hemolysis or platelet aggregation. In conclusion, the lipid-core nanocapsules uncoated or coated with chitosan are hemocompatible representing a potential innovative nanotechnological formulation for intravenous administration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biocompatible Materials*
  • Blood Coagulation / drug effects
  • Chemistry, Pharmaceutical
  • Chitosan / chemistry
  • Chitosan / toxicity*
  • Drug Carriers*
  • Drug Compounding
  • Erythrocyte Membrane / drug effects
  • Hemolysis / drug effects
  • Humans
  • Lecithins / chemistry
  • Lecithins / toxicity*
  • Light
  • Lipids / chemistry
  • Lipids / toxicity*
  • Materials Testing
  • Nanocapsules*
  • Nanotechnology
  • Partial Thromboplastin Time
  • Particle Size
  • Platelet Aggregation / drug effects
  • Polyesters / chemistry
  • Polyesters / toxicity*
  • Polysorbates / chemistry
  • Polysorbates / toxicity*
  • Prothrombin Time
  • Scattering, Radiation
  • Technology, Pharmaceutical / methods

Substances

  • Biocompatible Materials
  • Drug Carriers
  • Lecithins
  • Lipids
  • Nanocapsules
  • Polyesters
  • Polysorbates
  • polycaprolactone
  • Chitosan