Stealth nanoparticles coated with heparin as peptide or protein carriers

J Drug Target. 2009 Sep;17(8):575-85. doi: 10.1080/10611860903112909.

Abstract

Nanoparticles (prepared from a mixture of polyester and a polycationic polymer) loaded with insulin were prepared by a double emulsion method followed by evaporation solvent. Low molecular weight heparin (LMWH) was bound by electrostatic interactions onto the surface of the particles to confer Stealth properties. These nanoparticles were characterized in vitro (mean diameter, zeta potential, encapsulation efficiency, and release kinetics) and compared with conventional (without LMWH) and unloaded nanoparticles. The pharmacokinetics of insulin were studied after intravenous injection into diabetic rats in the form of Stealth or conventional nanoparticles or as a solution. Stealth nanoparticles allowed an increase in the elimination half-life of insulin, showing that the hydrophilic layer of LMWH was able to limit recognition by the mononuclear phagocytosis system in vivo. However, complement activation studies (CH50) did not reveal significant difference between Stealth and conventional nanoparticles.

Publication types

  • Comparative Study

MeSH terms

  • Acrylic Resins / chemistry
  • Animals
  • Diabetes Mellitus, Experimental / drug therapy
  • Drug Carriers / chemistry
  • Half-Life
  • Hypoglycemic Agents / administration & dosage*
  • Hypoglycemic Agents / pharmacokinetics
  • Hypoglycemic Agents / pharmacology
  • Injections, Intravenous
  • Insulin / administration & dosage*
  • Insulin / pharmacokinetics
  • Insulin / pharmacology
  • Insulin, Regular, Pork
  • Male
  • Mononuclear Phagocyte System / metabolism
  • Nadroparin / chemistry*
  • Nanoparticles*
  • Particle Size
  • Polyesters / chemistry
  • Polymers / chemistry
  • Rats
  • Rats, Wistar
  • Static Electricity

Substances

  • Acrylic Resins
  • Drug Carriers
  • Hypoglycemic Agents
  • Insulin
  • Insulin, Regular, Pork
  • Nadroparin
  • Polyesters
  • Polymers
  • polycaprolactone
  • Eudragit RS
  • insulin, neutral