title: 5-ASA loaded chitosan-Ca-alginate microparticles: Preparation and physicochemical characterization.
abstract: The objective of the work was to prepare chitosan-Ca-alginate microparticles that can effectively deliver 5-ASA to the colon after peroral administration. For these requirements, a spray-drying technique was applied to 5-ASA/sodium alginate aqueous solution to obtain spherical particles having a mean diameter less than 10microm. The microparticles formed were cross-linked and coated into solution of CaCl(2) and chitosan to obtain stable microsystem. (1)H NMR and UV-vis spectra of 5-ASA have shown no degradation when working in adequate conditions, such as light protection, freshly prepared solution and use of nitrogen to prevent the oxidative self-coupling of 5-ASA moieties. By imaging with SEM, acceptable spherical morphology was observed, but also flattened, disk-shaped particles of smooth surface and low porosity. CLSM imaging showed dominant localization of chitosan in the particle wall, while for alginate, a homogeneous distribution throughout the particle was observed giving the particles negative charge. In the FTIR spectra of 5-ASA loaded Ca-alginate microparticles the characteristic peaks of 5-ASA were not altered indicating no covalent interaction between the drug and the polymer. DSC and X-ray diffraction studies revealed that 5-ASA was molecularly dispersed within the chitosan-Ca-alginate microparticles during the production process.
authors.affiliation: Ss. Cyril and Methodious University, Faculty of Pharmacy, Vodnjanska 17, 1000 Skopje, Macedonia. krml@ff.ukim.edu.mk
authors.forename: K
authors.initials: K
authors.lastname: Mladenovska
authors.forename: O
authors.initials: O
authors.lastname: Cruaud
authors.forename: P
authors.initials: P
authors.lastname: Richomme
authors.forename: E
authors.initials: E
authors.lastname: Belamie
authors.forename: R S
authors.initials: RS
authors.lastname: Raicki
authors.forename: M-C
authors.initials: MC
authors.lastname: Venier-Julienne
authors.forename: E
authors.initials: E
authors.lastname: Popovski
authors.forename: J P
authors.initials: JP
authors.lastname: Benoit
authors.forename: K
authors.initials: K
authors.lastname: Goracinova
mesh_terms: D000464:Alginates / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D048271:Chitosan / Q000737:chemistry*; D003890:Desiccation; D004355:Drug Stability; D004563:Electrochemistry; D016650:Fluorescein-5-isothiocyanate; D005456:Fluorescent Dyes; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D019804:Mesalamine / Q000008:administration & dosage / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D010316:Particle Size; D014961:X-Ray Diffraction
chemical_list: D000464:Alginates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D005456:Fluorescent Dyes; D006603:Hexuronic Acids; D019804:Mesalamine; D020723:Glucuronic Acid; D048271:Chitosan; D016650:Fluorescein-5-isothiocyanate