PMID- 11102683 OWN - NLM STAT- MEDLINE DCOM- 20010118 LR - 20190915 IS - 0168-3659 (Print) IS - 0168-3659 (Linking) VI - 69 IP - 3 DP - 2000 Dec 3 TI - Protein encapsulation into biodegradable microspheres by a novel S/O/W emulsion method using poly(ethylene glycol) as a protein micronization adjuvant. PG - 435-44 AB - A new method for preparing protein-loaded biodegradable microspheres by a process involving solid-in-oil-in-water (S/O/W) emulsion was established using poly(ethylene glycol) (PEG). In the first step, a protein solution was lyophilized with PEG, which resulted in the formation of spherical protein microparticles, less than 5 microm in diameter, dispersed in a continuous PEG phase. This process was well explained by the aqueous phase separation phenomenon induced by freezing-condensation. Since this lyophilizate could be directly dispersed in an organic phase containing biodegradable polymer by dissolving PEG with methylene chloride, a conventional in-water drying method could be adopted in the second step. Through this S/O/W emulsion process, horseradish peroxidase was effectively entrapped into monolithic-type microspheres of poly(DL-lactic-co-glycolic acid) (PLGA), without significant loss of activity. Bovine superoxide dismutase (bSOD), as another model protein, could be encapsulated into reservoir-type microspheres by the 'polymer-alloys method' using both poly(DL-lactic acid) (PLA) and PLGA. The initial release of bSOD from this reservoir-type microsphere was efficiently reduced. Further, the bSOD release kinetics could be suitably modified by adjusting the loading amounts of PEG or polymer composition. In this study, the multi-functional nature of PEG was successfully utilized in the preparation and designing of protein-loaded microspheres. FAU - Morita, T AU - Morita T AD - DDS Research Department, Discovery Research Laboratory, Tanabe Seiyaku Co. Ltd., 3-16-89 Kashima, Yodogawa-ku, 532-8505, Osaka, Japan. t-morita@tanabe.com FAU - Sakamura, Y AU - Sakamura Y FAU - Horikiri, Y AU - Horikiri Y FAU - Suzuki, T AU - Suzuki T FAU - Yoshino, H AU - Yoshino H LA - eng PT - Journal Article PL - Netherlands TA - J Control Release JT - Journal of controlled release : official journal of the Controlled Release Society JID - 8607908 RN - 0 (Emulsions) RN - 0 (Polymers) RN - 0 (Proteins) RN - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer) RN - 26009-03-0 (Polyglycolic Acid) RN - 33X04XA5AT (Lactic Acid) RN - 3WJQ0SDW1A (Polyethylene Glycols) RN - EC 1.15.1.1 (Superoxide Dismutase) SB - IM MH - Animals MH - Cattle MH - *Emulsions MH - Lactic Acid/administration & dosage MH - Microspheres MH - Polyethylene Glycols MH - Polyglycolic Acid/administration & dosage MH - Polylactic Acid-Polyglycolic Acid Copolymer MH - Polymers/administration & dosage MH - Proteins/*administration & dosage MH - Superoxide Dismutase/administration & dosage MH - *Technology, Pharmaceutical EDAT- 2000/12/05 11:00 MHDA- 2001/02/28 10:01 CRDT- 2000/12/05 11:00 PHST- 2000/12/05 11:00 [pubmed] PHST- 2001/02/28 10:01 [medline] PHST- 2000/12/05 11:00 [entrez] AID - S0168365900003266 [pii] AID - 10.1016/s0168-3659(00)00326-6 [doi] PST - ppublish SO - J Control Release. 2000 Dec 3;69(3):435-44. doi: 10.1016/s0168-3659(00)00326-6.