title: pH-sensitive poly(lactide-co-glycolide) nanoparticle composite microcapsules for oral delivery of insulin.
abstract: This study proposes a new concept of pH-sensitive poly(lactide-co-glycolide) (PLGA) nanoparticle composite microcapsules for oral delivery of insulin. Firstly, insulin-sodium oleate complex was prepared by the hydrophobic ion pairing method and then encapsulated into PLGA nanoparticles by the emulsion solvent diffusion method. In order to reduce the burst release of insulin from PLGA nanoparticles and deliver insulin to specific gastrointestinal regions, hence to enhance bioavailability of insulin, the PLGA nanoparticles were further encapsulated into Eudragit(®) FS 30D to prepare PLGA nanoparticle composite microcapsules by organic spray-drying method. The preparation was evaluated in vitro and in vivo, and the absorption mechanism was discussed. The in vitro drug release studies revealed that the drug release was pH dependent, and the in vivo results demonstrated that the formulation of PLGA nanoparticle composite microcapsules was an effective candidate for oral insulin delivery.
authors.affiliation: Key Laboratory of Chemical Engineering Process and Technology for High-efficiency Conversion, College of Heilongjiang Province (Heilongjiang University), School of Chemistry and Material Science, Heilongjiang University, Harbin, People's Republic of China.
authors.forename: Shaoping
authors.initials: S
authors.lastname: Sun
authors.affiliation: College of Chemistry and Chemical Engineering, Harbin Normal University, Harbin, People's Republic of China.
authors.forename: Na
authors.initials: N
authors.lastname: Liang
authors.affiliation: School of Pharmaceutical Science, Aichi Gakuin University, Nissin, Japan.
authors.forename: Hiromitsu
authors.initials: H
authors.lastname: Yamamoto
authors.affiliation: School of Pharmaceutical Science, Aichi Gakuin University, Nissin, Japan.
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Kawashima
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
authors.forename: Fude
authors.initials: F
authors.lastname: Cui
authors.affiliation: Key Laboratory of Chemical Engineering Process and Technology for High-efficiency Conversion, College of Heilongjiang Province (Heilongjiang University), School of Chemistry and Material Science, Heilongjiang University, Harbin, People's Republic of China ; Key Laboratory of Functional Inorganic Material Chemistry, Heilongjiang University, Harbin, People's Republic of China.
authors.forename: Pengfei
authors.initials: P
authors.lastname: Yan
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002214:Capsules / Q000008:administration & dosage / Q000737:chemistry; D004337:Drug Carriers; D007328:Insulin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017208:Rats, Wistar
chemical_list: D002214:Capsules; D004337:Drug Carriers; D007328:Insulin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid
keywords: Eudragit® FS 30D; PLGA nanoparticles; complex; sodium oleate