title: pH-responsive release of proteins from biocompatible and biodegradable reverse polymer micelles.
abstract: A reverse polymer micelle with a diameter of 100nm was prepared for a protein carrier releasing payloads in a pH-dependent manner. The reverse polymer micelle was made from an amphiphilic diblock copolymer of biodegradable poly(d,l-lactic-co-glycolic acid) (PLGA) and biocompatible poly(ethylene glycol) (PEG). PLGA having a terminal carboxyl group was additionally embedded in the micelle's PLGA layer via hydrophobic interaction. The micelles encapsulating bovine serum albumin and streptavidin released the proteins under neutral and basic conditions, whereas the proteins remained in the interior at acidic pH. Using erythropoietin as a protein drug, it was also exemplified that the released protein retained its cell proliferation activity even after rigorous formulation processes, including water-in-oil emulsion. The present reverse polymer micelle could potentially find application as an oral protein drug delivery carrier.
authors.affiliation: New Frontiers Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan; Bioengineering Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan. Electronic address: Yuichi_Koyamatsu@nts.toray.co.jp.
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Koyamatsu
authors.affiliation: New Frontiers Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan.
authors.forename: Taisuke
authors.initials: T
authors.lastname: Hirano
authors.affiliation: New Frontiers Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan.
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Kakizawa
authors.affiliation: New Frontiers Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan.
authors.forename: Fumiyoshi
authors.initials: F
authors.lastname: Okano
authors.affiliation: Bioengineering Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan. Electronic address: ttkrd@riken.jp.
authors.forename: Tohru
authors.initials: T
authors.lastname: Takarada
authors.affiliation: Bioengineering Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
authors.forename: Mizuo
authors.initials: M
authors.lastname: Maeda
mesh_terms: D000818:Animals; D001672:Biocompatible Materials / Q000737:chemistry; D002417:Cattle; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004921:Erythropoietin / Q000008:administration & dosage*; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D019344:Lactic Acid / Q000737:chemistry*; D008823:Micelles; D010743:Phospholipids / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012710:Serum Albumin, Bovine / Q000008:administration & dosage*
chemical_list: D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D008823:Micelles; D010743:Phospholipids; D004921:Erythropoietin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D012710:Serum Albumin, Bovine; D019344:Lactic Acid; D011092:Polyethylene Glycols
keywords: Biocompatible; Biodegradable; Biopharmaceutical; Erythropoietin; Reverse polymer micelle; pH