title: Genipin-structured peptide-polysaccharide nanoparticles with significantly improved resistance to harsh gastrointestinal environments and their potential for oral delivery of polyphenols.
abstract: Genipin-cross-linked caseinophosphopeptide (CPP)-chitosan (CS) nanoparticles (smaller than 300 nm) showed significantly improved stability and adjustable release profile in the gastrointestinal (GI) tract. Optimal purification of the nanoparticles was established by centrifugation to terminate the cross-linking reaction, which was further confirmed and characterized by FT-IR. Results from transmission electron microscopy (TEM), dynamic light scattering (DLS), and electrophoretic mobility (ζ-potential) measurements revealed that genipin cross-linking significantly prevented the bursting of the CPP-CS nanoparticles in simulated stomach acid and their precipitation under neutral intestinal environment. Pepsin showed little impact on the nanoparticle colloid stability; however, trypsin induced their aggregations. Genipin cross-linking slowed the burst release of (-)-epigallocatechin-3-gallate (EGCG) from the nanoparticles. The EGCG-loaded nanoparticles showed strong cytotoxicity against cancer cells; meanwhile, the net nanoparticles demonstrated high biocompatibility. The findings in the present work provide fundamental information for the rational design of biopolymer nanoparticles as an effective delivery systems for polyphenols.
authors.affiliation: College of Food Science and Technology, Nanjing Agricultural University , Nanjing 210095, People's Republic of China.
authors.forename: Bing
authors.initials: B
authors.lastname: Hu
authors.forename: Minhao
authors.initials: M
authors.lastname: Xie
authors.forename: Chen
authors.initials: C
authors.lastname: Zhang
authors.forename: Xiaoxiong
authors.initials: X
authors.lastname: Zeng
mesh_terms: D002364:Caseins / Q000737:chemistry* / Q000378:metabolism; D002392:Catechin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D041981:Gastrointestinal Tract / Q000378:metabolism*; D006801:Humans; D039823:Iridoids / Q000737:chemistry* / Q000378:metabolism; D053758:Nanoparticles / Q000737:chemistry / Q000378:metabolism; D010446:Peptide Fragments / Q000737:chemistry* / Q000378:metabolism; D059808:Polyphenols / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D011509:Proteoglycans / Q000737:chemistry* / Q000378:metabolism
chemical_list: D002364:Caseins; D004337:Drug Carriers; D039823:Iridoids; D010446:Peptide Fragments; D059808:Polyphenols; D011509:Proteoglycans; C065989:caseinomacropeptide; C093216:polysaccharide peptide; D002392:Catechin; D048271:Chitosan; C007834:genipin; C045651:epigallocatechin gallate
keywords: EGCG; biopolymer nanoparticles; centrifugal purification; controlled release; genipin; oral delivery; structure behavior