Water-free microencapsulation of proteins within PLGA microparticles by spray drying using PEG-assisted protein solubilization technique in organic solvent.
Poly(d,l-lactic-co-glycolic acid) (PLGA) microparticles encapsulating therapeutic proteins were prepared under a water-free formulation condition. Bovine serum albumin (BSA) and recombinant human growth hormone (rhGH) were homogeneously solubilized as nano-scale complexes in methylene chloride phase by using polyethylene glycol (PEG) as a complex-forming agent. The organic phase containing dissolved PLGA and PEG/protein complexes was directly spray dried to obtain PLGA microparticles encapsulating proteins. They exhibited sustained release profiles of BSA and rhGH up to 30 days with reduced initial bursts. The released protein molecules from the microparticles maintained structural integrity without aggregation, suggesting that the current single-step protein microencapsulation method without using water could be potentially applied for sustained delivery of a wide range of therapeutic protein drugs that are not soluble in organic solvents.
Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon, South Korea.
Hyejung
H
Mok
Tae Gwan
TG
Park
D000818:Animals; D002417:Cattle; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D003890:Desiccation; D004337:Drug Carriers; D004339:Drug Compounding; D019382:Human Growth Hormone / Q000737:chemistry; D006801:Humans; D007700:Kinetics; D019344:Lactic Acid / Q000737:chemistry*; D008752:Methylene Chloride / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011506:Proteins / Q000737:chemistry*; D011994:Recombinant Proteins / Q000737:chemistry; D012710:Serum Albumin, Bovine / Q000737:chemistry; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods*; D014867:Water / Q000737:chemistry
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011506:Proteins; D011994:Recombinant Proteins; D012997:Solvents; D014867:Water; D019382:Human Growth Hormone; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D012710:Serum Albumin, Bovine; D019344:Lactic Acid; D011092:Polyethylene Glycols; D008752:Methylene Chloride