title: Characteristics and release profiles of MPEG-PCL-MPEG microspheres containing immunoglobulin G.
abstract: Polyester-polyether type block copolymers have attracted attention in the area of drug delivery systems with their capability in providing a broad range of amphiphilic characteristics. The aim of the present work was to prepare and characterize immunoglobulin G (IgG) loaded methoxy poly(ethylene glycol)-poly(ɛ-caprolactone)-methoxy poly(ethylene glycol) (MPEG-PCL-MPEG) microspheres as potential carrier for therapeutic monoclonal antibodies used in clinics. MPEG-PCL-MPEG triblock copolymer was synthesized by ring-opening polymerization of ɛ-caprolactone initiated by MPEG and then characterized. Microspheres were prepared by double emulsion-solvent evaporation method and their properties were compared with those of PCL microspheres. Microspheres had spherical shape with a mean particle size around 6 μm. MPEG-PCL-MPEG microspheres had higher encapsulation efficiency than PCL microspheres. After 90 days of release, 30±2% and 57±3% of the bioactivity of IgG released from non-irradiated PCL and MPEG-PCL-MPEG microspheres were protected, respectively. Presence of MPEG in microspheres provided more controlled IgG release rate and protected IgG from denaturation during γ-irradiation (20±3% and 49±2% for PCL and MPEG-PCL-MPEG microspheres, respectively). In vitro cytotoxicity tests revealed that both MPEG-PCL-MPEG and PCL microspheres had no toxic effect on cells. This study showed that MPEG-PCL-MPEG microspheres are promising delivery systems for therapeutic monoclonal antibodies.
authors: Department of Engineering Sciences, Middle East Technical University, Ankara, Turkey.
authors: Özge
authors: Ö
authors: Erdemli
authors: Department of Chemistry, Middle East Technical University, Ankara, Turkey.
authors: Ali
authors: A
authors: Usanmaz
authors: Department of Engineering Sciences, Middle East Technical University, Ankara, Turkey; Biomaterials and Tissue Engineering Center of Excellence, Middle East Technical University, Ankara, Turkey.
authors: Dilek
authors: D
authors: Keskin
authors: Department of Engineering Sciences, Middle East Technical University, Ankara, Turkey; Biomaterials and Tissue Engineering Center of Excellence, Middle East Technical University, Ankara, Turkey. Electronic address: tezcaner@metu.edu.tr.
authors: Ayşen
authors: A
authors: Tezcaner
mesh_terms: D016475:3T3 Cells; D000818:Animals; D005720:Gamma Rays; D006801:Humans; D007074:Immunoglobulin G / Q000378:metabolism*; D007700:Kinetics; D051379:Mice; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D008970:Molecular Weight; D010316:Particle Size; D011091:Polyesters / Q000138:chemical synthesis / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000138:chemical synthesis / Q000737:chemistry*; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D007074:Immunoglobulin G; D011091:Polyesters; C000593606:methoxy poly(ethylene glycol)-poly(epsilon-caprolactone)-methoxy poly(ethylene glycol); D011092:Polyethylene Glycols
keywords: Amphiphilic triblock copolymer; Methoxy poly(ethylene glycol)-poly(ɛ-caprolactone)-methoxy poly(ethylene glycol); Microspheres; Polymeric drug delivery; Protein delivery; γ-sterilization