Pegylated recombinant human epidermal growth factor (rhEGF) for sustained release from biodegradable PLGA microspheres.
Recombinant human epidermal growth factor (rhEGF) was conjugated with polyethylene glycol (PEG) to improve its physical stability during microencapsulation in biodegradable poly(lactic-co-glycolic acid) microspheres. rhEGF was conjugated with N-hydroxysuccimide (NHS)-derivatized methoxy-PEG (mPEG) of MW 2000 and 5000 under various reaction conditions to optimize the extent of pegylation. Pegylated rhEGF showed much enhanced physical stability against homogenization. Pegylated rhEGF was encapsulated in PLGA microspheres by a double emulsion solvent evaporation method to achieve a sustained release. Pegylated rhEGF exhibited a tri-phasic release profile with a reduced initial burst, compared with unpegylated rhEGF. This study demonstrated that protein pegylation enhanced physical stability of protein and could be a good approach to achieve a sustained protein release profile from biodegradable microspheres.
Kim
Tae Hyoung
TH
Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Taejon, South Korea.
Lee
Haeshin
H
Park
Tae Gwan
TG
D000595:Amino Acid Sequence; D001672:Biocompatible Materials; D001673:Biodegradation, Environmental; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D004355:Drug Stability; D004815:Epidermal Growth Factor / Q000008:administration & dosage* / Q000737:chemistry / Q000235:genetics; D006801:Humans; D066298:In Vitro Techniques; D019344:Lactic Acid; D008422:Materials Testing; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D008969:Molecular Sequence Data; D008970:Molecular Weight; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers; D011994:Recombinant Proteins / Q000008:administration & dosage / Q000737:chemistry / Q000235:genetics
D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D011108:Polymers; D011994:Recombinant Proteins; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D004815:Epidermal Growth Factor