Polyelectrolyte complex nanoparticles based on chitosan and methoxy poly(ethylene glycol) methacrylate-co-poly(methylacrylic acid) for oral delivery of ibuprofen

Colloids Surf B Biointerfaces. 2018 May 1:165:235-242. doi: 10.1016/j.colsurfb.2018.02.037. Epub 2018 Feb 21.

Abstract

In this study, the copolymer of methoxy poly(ethylene glycol) methacrylate-co-poly(methylacrylic acid) [poly(mPEGMA-co-MAA)] was synthesized via radical polymerization. Based on this copolymer, novel chitosan-modified poly(mPEGMA-co-MAA) nanoparticles (CS/NPs) were developed to improve the bio-availability of ibuprofen (IBU). Fourier transform infrared spectroscopy (FTIR) and 1H nuclear magnetic resonance (1H NMR) spectra were used to confirm the synthesis of the copolymers. The morphology of CS/NPs was investigated with transmission electron microscopy (TEM). Thermogravimetric analysis (TGA) was used to reveal the thermodynamic properties of the CS/NPs. The cytotoxicity of CS/NPs was assessed by the cell viability of 293T cells. FTIR and 1H NMR spectra confirmed the synthesis of the novel copolymer. TEM photographs showed that the CS/NPs had a core-shell structure. High cell viability indicated that the CS/NPs were nontoxic. The in vitro release profiles suggested that the CS/NPs released IBU in pH 7.4 buffer in a continuous manner. Furthermore, the IBU-CS/NPs showed a long antifebrile effect. Animal experiments showed that the IBU-CS/NPs had obvious antifebrile effects. Therefore, CS/NPs could reduce the dosing frequency of IBU, and improve its bio-availability.

Keywords: Cell uptake; Chitosan; Cytotoxicity; Ibuprofen; Poly(mPEGMA-co-MAA).

MeSH terms

  • Acrylates / chemistry
  • Administration, Oral
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Cell Survival / drug effects
  • Chitosan / chemistry*
  • Disease Models, Animal
  • Drug Carriers*
  • Drug Liberation
  • Fever / chemically induced
  • Fever / drug therapy*
  • Fever / physiopathology
  • HEK293 Cells
  • Humans
  • Hydrogen-Ion Concentration
  • Ibuprofen / chemistry
  • Ibuprofen / pharmacology*
  • Injections, Subcutaneous
  • Methacrylates / chemistry*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Polyethylene Glycols / chemistry*
  • Rats
  • Rats, Sprague-Dawley
  • Thermodynamics
  • Yeast, Dried / administration & dosage

Substances

  • Acrylates
  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Methacrylates
  • methoxy polyethylene glycol methacrylate
  • Polyethylene Glycols
  • Chitosan
  • methyl acrylate
  • Ibuprofen