The ability of poloxamers to inhibit platelet aggregation depends on their physicochemical properties

Thromb Haemost. 2001 Dec;86(6):1532-9.

Abstract

Poloxamers, block copolymers of polyethylene glycol (PEG) and polypropylene glycol (PPG), are thought to reduce cell-cell adhesion during vascular disorders. We examined how the amphiphilic nature of these polymers may contribute to their ability to inhibit ADP-induced platelet aggregation. Four Poloxamers (184, 188, 335 and 338) with varying PEG and PPG block lengths were examined. Of these, Poloxamer 184 at 2 mM markedly inhibited platelet aggregation. We observed that: i) Typically, less than 10% of the platelet surface is covered by Poloxamers, and greater than 99% of the polymer either remains in solution or binds soluble components in blood plasma. ii) Increasing the PEG side-chain length does not significantly augment the ability of Polox-amers to inhibit platelet aggregation. iii) Poloxamer 184, but not Polox-amers 188 and 335, significantly reduces the ability of stimulated platelets to bind fibrinogen and antibody PAC-1. The study demonstrates that the physical adsorption of some Poloxamers may allow them to inhibit platelet aggregation. The inhibition mechanism involves either binding of Poloxamers to platelet GPIIb-IIIa or inhibition of cellular activation pathways.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Adenosine Diphosphate / antagonists & inhibitors
  • Adenosine Diphosphate / pharmacology
  • Adsorption
  • Antibodies, Monoclonal / metabolism
  • Calorimetry, Differential Scanning
  • Drug Evaluation, Preclinical
  • Fibrinogen / metabolism
  • Humans
  • Kinetics
  • Micelles
  • Microspheres
  • Molecular Weight
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / pharmacology*
  • Platelet Glycoprotein GPIIb-IIIa Complex / antagonists & inhibitors
  • Platelet Glycoprotein GPIIb-IIIa Complex / metabolism
  • Poloxamer / chemistry
  • Poloxamer / pharmacology*
  • Protein Binding
  • Solubility
  • Structure-Activity Relationship
  • Surface Properties
  • Viscosity

Substances

  • Antibodies, Monoclonal
  • Micelles
  • Platelet Aggregation Inhibitors
  • Platelet Glycoprotein GPIIb-IIIa Complex
  • Poloxamer
  • Adenosine Diphosphate
  • Fibrinogen