5-ASA loaded chitosan-Ca-alginate microparticles: Preparation and physicochemical characterization.
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.
Mladenovska
K
K
Ss. Cyril and Methodious University, Faculty of Pharmacy, Vodnjanska 17, 1000 Skopje, Macedonia. krml@ff.ukim.edu.mk
Cruaud
O
O
Richomme
P
P
Belamie
E
E
Raicki
R S
RS
Venier-Julienne
M-C
MC
Popovski
E
E
Benoit
J P
JP
Goracinova
K
K
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
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