Protein C-loaded monomethoxypoly (ethylene oxide)-poly(lactic acid) nanoparticles

Int J Pharm. 2001 Jan 5;212(1):1-9. doi: 10.1016/s0378-5173(00)00548-2.

Abstract

This paper deals with the preparation and characterization of monomethoxypoly(ethylene oxide)-poly(lactic acid) (MPEO-PLA) nanoparticles containing protein C, a plasma inhibitor which regulates the mechanism of blood coagulation. Protein C was entrapped in MPEO-PLA nanoparticles using the double emulsion method. The influence of MPEO-PLA copolymers on the different parameters was evaluated: characteristics of protein C-loaded nanoparticles, in vitro release of the protein, evolution of the particle size with incubation time and MPEO release. The nanoparticle size does not depend on copolymer characteristics (MPEO and/or PLA block molecular weight). On the other hand, the efficiency of protein C entrapment is affected by the copolymer characteristics. The burst effect during the protein C release is increased with the hydrophilic character of the copolymer. Moreover, protein C adsorption on the particle surface during its release may be related to MPEO release. Only 25% of the released protein C is active, which clearly illustrates that it is altered during its encapsulation. The optimization of the experimental parameters which disturbed entrapped protein C activity, i.e. sonication time and organic solvent was investigated and has led to a preservation of protein C activity. Then, to optimize its entrapment efficiency, a blend PLA/MPEO-PLA (25/75) was used to prepare nanoparticles. This blend limited burst effect of protein C and its adsorption. However, protein C is only partially released which implicates further investigation for a potential therapeutic use.

MeSH terms

  • Lactates / administration & dosage*
  • Lactates / chemistry
  • Particle Size
  • Polyethylene Glycols / administration & dosage*
  • Polyethylene Glycols / chemistry
  • Polymers / administration & dosage*
  • Polymers / chemistry
  • Protein C / administration & dosage*
  • Protein C / chemistry

Substances

  • Lactates
  • Polymers
  • Protein C
  • polyethylene oxide-polylactic acid block copolymer
  • Polyethylene Glycols