title: Microencapsulation of beta-galactosidase with Eudragit L-100.
abstract: Microcapsules containing beta-galactosidase (lactase) were prepared by solvent evaporation using the pH sensitive polymer, Eudragit L-100. Formulations were prepared using various polymer-enzyme ratios with total solids content of the internal phase using sucrose stearate as a droplet stabilizer. Particle size distributions were invariant to relative proportion of ingredients but were dependent on stirring conditions. Although sucrose stearate had no effect on particle size distribution, release rate or encapsulation efficiency, its presence at a minimum 2% level was necessary to ensure intact microcapsules. Encapsulation efficiencies were higher for formulations prepared with 15% compared to 10% total solid content. DSC results revealed an interaction between encapsulated Eudragit L-100-enzyme-sucrose stearate vs their physical mixtures. The enzyme activities of the freshly prepared product vs those stored under stressed condition (40 degrees C and 75% RH) were 68 and 40% of their pre-processing activity, respectively. In vitro dissolution showed no enzyme release at 1 h in acidic media but 80% of the lactase was released from the microcapsules over 2.5 h in pH 6.8 media, thus establishing the feasibility of lactase microencapsulation to retard enzyme release in an acidic environment and ensuring release at intestinal pH.
authors.affiliation: College of Pharmacy, St John's University, 8000 Utopia Parkway, Jamaica, NY 11439, USA. squillae@stjohns.edu
authors.forename: E
authors.initials: E
authors.lastname: Squillante
authors.forename: G
authors.initials: G
authors.lastname: Morshed
authors.forename: S
authors.initials: S
authors.lastname: Bagchi
authors.forename: K A
authors.initials: KA
authors.lastname: Mehta
mesh_terms: D002151:Calorimetry / Q000379:methods; D002214:Capsules; D004339:Drug Compounding / Q000379:methods; D006863:Hydrogen-Ion Concentration; D008855:Microscopy, Electron, Scanning; D011109:Polymethacrylic Acids / Q000737:chemistry* / Q000493:pharmacokinetics; D012995:Solubility; D013228:Stearates / Q000494:pharmacology; D013395:Sucrose / Q000494:pharmacology; D001616:beta-Galactosidase / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D002214:Capsules; D011109:Polymethacrylic Acids; D013228:Stearates; C038300:methylmethacrylate-methacrylic acid copolymer; D013395:Sucrose; D001616:beta-Galactosidase