Long acting porous microparticle for pulmonary protein delivery.
This study investigated the porous-microparticle (PM) with low mass density and large size for pulmonary drug delivery. PM was prepared by the water-in-oil-in-water (W(1)/O/W(2)) multi-emulsion method with cyclodextrin derivative as a porogen and a stabilizer of peptide drugs. Herein, sucrose ethyl acetate (SAIB) was incorporated in PM for long acting protein release. In vitro release studies, the rapid release rate of proteins from PM was reduced due to the high viscosity of the added SAIB. As a result, BSA release from PM continued up to 7 days. This result suggests that PM having sustained release characteristics may be successfully applied for long-term pulmonary administration of protein or peptide drug. In addition, it is expected that these particles arrive at a deep lung epithelium due to low density (high porosity) and limit macrophage recognition because of big particle size (more than 5 microm).
Kwon
Min Jung
MJ
Pharmaceutical and Health Research Institute, Amore Pacific Corporation/R&D Center, 314-1, Bora-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-729, Republic of Korea.
Bae
Jun Ho
JH
Kim
Jung Ju
JJ
Na
Kun
K
Lee
Eun Seong
ES
D000280:Administration, Inhalation; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D004655:Emulsions; D007700:Kinetics; D019344:Lactic Acid / Q000737:chemistry*; D008863:Microspheres; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry*; D016062:Porosity; D011506:Proteins / Q000008:administration & dosage / Q000737:chemistry*; D012710:Serum Albumin, Bovine / Q000737:chemistry; D012995:Solubility; D013395:Sucrose / Q000031:analogs & derivatives / Q000737:chemistry*; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D014783:Viscosity; D014867:Water / Q000737:chemistry; D047392:beta-Cyclodextrins / Q000737:chemistry*
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D009821:Oils; D011108:Polymers; D011506:Proteins; C103513:SBE7-beta-cyclodextrin; D047392:beta-Cyclodextrins; D014867:Water; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D012710:Serum Albumin, Bovine; D019344:Lactic Acid; D013395:Sucrose