title: Co-loading and intestine-specific delivery of multiple antioxidants in pH-responsive microspheres based on TEMPO-oxidized polysaccharides.
abstract: In this study, pH-responsive microspheres loaded with multiple antioxidants were developed for intestine-specific delivery and exhibited synergistic activity. They consist of chitosan (CS)-coated microspheres made of TEMPO-oxidized Konjac glucomannan (OKGM) polymers, of which the carboxyl (COO-) groups are cross-linked via ferric ions (Fe3+), allowing the hydrophobic (β-carotene) and hydrophilic (anthocyanins) antioxidants to be simultaneously incorporated. CLSM images showed successful co-encapsulation of β-carotene and anthocyanins. The in vitro release kinetics of co-loaded CS-OKGM microspheres in simulated GI fluids indicated that the microspheres retain the dual antioxidants in an acidic gastric environment and release them at intestinal pH. Free radical scavenging experiments demonstrated that multiple antioxidants loaded into OKGM system had synergistic activity with enhanced stability against heat. The multi-functional CS-OKGM microspheres showed great potential for multiple antioxidants and intestine-specific delivery with enhanced stability.
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, Key Laboratory of Functional Dairy, College of Food Science and Nutritional Engineering, China Agricultural University, 100083, China; College of Life Science and Technology, Beijing University of Chemical Technology, 100029, Beijing, China.
authors.forename: Mengxuan
authors.initials: M
authors.lastname: Shi
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, Key Laboratory of Functional Dairy, College of Food Science and Nutritional Engineering, China Agricultural University, 100083, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Bai
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, Key Laboratory of Functional Dairy, College of Food Science and Nutritional Engineering, China Agricultural University, 100083, China.
authors.forename: Liyun
authors.initials: L
authors.lastname: Zhao
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, Key Laboratory of Functional Dairy, College of Food Science and Nutritional Engineering, China Agricultural University, 100083, China.
authors.forename: Xinrui
authors.initials: X
authors.lastname: Yu
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, Key Laboratory of Functional Dairy, College of Food Science and Nutritional Engineering, China Agricultural University, 100083, China.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Liang
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, Key Laboratory of Functional Dairy, College of Food Science and Nutritional Engineering, China Agricultural University, 100083, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Laboratory of Physical Chemistry and Soft Matter, Wageningen University, Dreijenplein 6, 6703 HB, Wageningen, The Netherlands.
authors.forename: Willem
authors.initials: W
authors.lastname: Nord
authors.affiliation: Beijing Advanced Innovation Center for Food Nutrition and Human Health, Key Laboratory of Functional Dairy, College of Food Science and Nutritional Engineering, China Agricultural University, 100083, China. Electronic address: yuanli@cau.edu.cn.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Li
mesh_terms: D000872:Anthocyanins / Q000008:administration & dosage; D000975:Antioxidants / Q000008:administration & dosage*; D003497:Cyclic N-Oxides; D004337:Drug Carriers / Q000737:chemistry*; D057809:HEK293 Cells; D006801:Humans; D007422:Intestines; D008863:Microspheres; D011134:Polysaccharides / Q000737:chemistry*; D019207:beta Carotene / Q000008:administration & dosage
chemical_list: D000872:Anthocyanins; D000975:Antioxidants; D003497:Cyclic N-Oxides; D004337:Drug Carriers; D011134:Polysaccharides; D019207:beta Carotene; C003959:TEMPO
keywords: 2,2,6,6-Tetramethyl-1-piperidinyloxy (PubChem CID: 2724126); 2,2-Di(4-Tert-octylphenyl)-1-picrylhydrazyl (PubChem CID: 16211728); Beta-carotene (PubChem CID: 5280489); Chitosan (PubChem CID: 71853); Ferrous sulphate (PubChem CID: 24393); Fluorescein isothiocyanate (PubChem CID: 18730); Konjac glucomannan microspheres; Multiple antioxidants delivery; Oral delivery system; Sodium hydroxide (PubChem CID: 14789); Sodium hypochlorite (PubChem CID: 23665760); TEMPO-oxidation; pH-responsive microspheres