title: Pectin-coated chitosan-LDH bionanocomposite beads as potential systems for colon-targeted drug delivery.
abstract: This work introduces results on a new drug delivery system (DDS) based on the use of chitosan/layered double hydroxide (LDH) biohybrid beads coated with pectin for controlled release in the treatment of colon diseases. Thus, the 5-aminosalicylic acid (5ASA), the most used non-steroid-anti-inflammatory drug (NSAID) in the treatment of ulcerative colitis and Crohn's disease, was chosen as model drug aiming to a controlled and selective delivery in the colon. The pure 5ASA drug and the hybrid material prepared by intercalation in a layered double hydroxide of Mg2Al using the co-precipitation method, were incorporated in a chitosan matrix in order to profit from its mucoadhesiveness. These compounds processed as beads were further treated with the polysaccharide pectin to create a protective coating that ensures the stability of both chitosan and layered double hydroxide at the acid pH of the gastric fluid. The resulting composite beads presenting the pectin coating are stable to water swelling and procure a controlled release of the drug along their passage through the simulated gastrointestinal tract in in vitro experiments, due to their resistance to pH changes. Based on these results, the pectin@chitosan/LDH-5ASA bionanocomposite beads could be proposed as promising candidates for the colon-targeted delivery of 5ASA, with the aim of acting only in the focus of the disease and minimizing side effects.
authors.affiliation: Instituto de Ciencia de Materiales de Madrid, CSIC, Cantoblanco, 28049 Madrid, Spain; Universidade Federal de São Carlos, Monjolinho, 13565-905 São Carlos, SP Brazil.
authors.forename: Lígia N M
authors.initials: LN
authors.lastname: Ribeiro
authors.affiliation: Instituto de Ciencia de Materiales de Madrid, CSIC, Cantoblanco, 28049 Madrid, Spain.
authors.forename: Ana C S
authors.initials: AC
authors.lastname: Alcântara
authors.affiliation: Instituto de Ciencia de Materiales de Madrid, CSIC, Cantoblanco, 28049 Madrid, Spain.
authors.forename: Margarita
authors.initials: M
authors.lastname: Darder
authors.affiliation: Instituto de Ciencia de Materiales de Madrid, CSIC, Cantoblanco, 28049 Madrid, Spain.
authors.forename: Pilar
authors.initials: P
authors.lastname: Aranda
authors.affiliation: Universidade Federal de São Carlos, Monjolinho, 13565-905 São Carlos, SP Brazil.
authors.forename: Fernando M
authors.initials: FM
authors.lastname: Araújo-Moreira
authors.affiliation: Instituto de Ciencia de Materiales de Madrid, CSIC, Cantoblanco, 28049 Madrid, Spain. Electronic address: eduardo@icmm.csic.es.
authors.forename: Eduardo
authors.initials: E
authors.lastname: Ruiz-Hitzky
mesh_terms: D048271:Chitosan / Q000737:chemistry*; D003106:Colon / Q000378:metabolism; D016503:Drug Delivery Systems; D006878:Hydroxides / Q000737:chemistry*; D019804:Mesalamine / Q000737:chemistry; D009077:Mucins / Q000737:chemistry; D053761:Nanocomposites / Q000737:chemistry*; D010368:Pectins / Q000737:chemistry*
chemical_list: D006878:Hydroxides; D009077:Mucins; D019804:Mesalamine; D010368:Pectins; D048271:Chitosan
keywords: 5-aminosalicylic acid; 5-aminosalicylic acid (PubChemCID: 4075); AlCl(3)·6H(2)O (PubChemCID: 24564); Bionanocomposites; CaCl(2)·2H(2)O (PubChemCID: 24854).; Chitosan; Chitosan from crab shells (PubChemCID: 71853); Drug delivery systems; Layered double hydroxide; MgCl(2)·6H(2)O (PubChemCID: 24644); Pectin; mucin from porcine stomach (PubChemCID: 124890); pectin from citrus fruits (PubChemCID: 441476)