title: Antioxidant encapsulated porous poly(lactide-co-glycolide) microparticles for developing long acting inhalation system.
abstract: The purpose of this study was to fabricate porous poly(lactide-co-glycolide) (PLGA) microparticles for efficient pulmonary deposition and increased therapeutic duration of the antioxidant anthocyanin (ATH). These microparticles were prepared by a water-in-oil-in-water (W(1)/O/W(2)) multi-emulsion method with vaporizing ammonium bicarbonate (AB) as a porogen and starch as a viscous additive. High porosity achieved by the decomposition reaction of AB to the base of ammonia, carbon dioxide, and water vapor at 50°C enabled efficient deposition of ATH throughout the entire lung in BALB/c mice. In addition, the porous microparticles incorporating starch showed sustained ATH release characteristics (up to 5 days) and protracted antioxidant activity (up to 5 days) for 2,2-diphenyl-1-pikryl-hydrazyl (DPPH) radicals, which was comparable to that of the porous microparticles without starch which completely released ATH in 2h. Furthermore, these porous microparticles incorporating starch led to longer ATH residence (up to 20 days) in in vivo lung epithelium. We believe that this system has great pharmaceutical potential as a long-acting antioxidant for continuously relieving oxidative stress in pulmonary diseases like chronic obstructive pulmonary disease (COPD).
authors.affiliation: Division of Biotechnology, The Catholic University of Korea, Wonmi-gu, Bucheon-si, Gyeonggi-do, Republic of Korea.
authors.forename: Na Young
authors.initials: NY
authors.lastname: Yoo
authors.forename: Yu Seok
authors.initials: YS
authors.lastname: Youn
authors.forename: Nam Muk
authors.initials: NM
authors.lastname: Oh
authors.forename: Kyung Taek
authors.initials: KT
authors.lastname: Oh
authors.forename: Deok-Keun
authors.initials: DK
authors.lastname: Lee
authors.forename: Kyung-Hoi
authors.initials: KH
authors.lastname: Cha
authors.forename: Young Taik
authors.initials: YT
authors.lastname: Oh
authors.forename: Eun Seong
authors.initials: ES
authors.lastname: Lee
mesh_terms: D000280:Administration, Inhalation; D000818:Animals; D000872:Anthocyanins / Q000737:chemistry / Q000627:therapeutic use; D000975:Antioxidants / Q000737:chemistry* / Q000627:therapeutic use; D002460:Cell Line; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D005260:Female; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008168:Lung / Q000378:metabolism*; D051379:Mice; D008807:Mice, Inbred BALB C; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D016062:Porosity; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy
chemical_list: D000872:Anthocyanins; D000975:Antioxidants; D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid