title: In vitro evaluation of coating polymers for enteric coating and human ileal targeting.
abstract: Recombinant interleukin-10 producing Lactococcus lactis is an alternative therapy for Crohn's disease. For in vivo interleukin-10 production, thymidine, the essential feed component of these recombinant bacteria should be coadministered. Different coating polymers were evaluated in vitro for enteric properties and targeting suitability to the ileum, the major site of inflammation in Crohn's disease. To guarantee ileal delivery, the polymer must dissolve from pH 6.8 and allow complete release within 40 min. Aqoat AS-HF coated pellets (15%) showed poor enteric properties and thymidine was released below pH 6.8. Eudragit FS30D coated pellets (15%) showed good enteric properties, but no thymidine was released within 40 min at pH 6.8. Eudragit S coated pellets (15%) showed good enteric properties after curing at elevated temperature while no thymidine was released within 40 min at pH 6.8. In another approach to pass the proximal small intestine intact, pellets were coated with 30% Eudragit L30D-55. At pH 6.0, they showed a lag-phase of 20 min. No influence of layer thickness was seen above pH 6.5. Alternatively, pellets were coated with a mixture of Eudragit FS30D/L30D-55 but they showed poor enteric properties and thymidine was released below pH 6.8. In conclusion, none of the tested polymers/mixtures ensured enteric properties and ileal targeting.
authors.affiliation: Laboratory of Pharmaceutical Technology, Ghent University, Faculty of Pharmaceutical Science, Harelbekestraat 72, B-9000, Ghent, Belgium.
authors.forename: Nathalie
authors.initials: N
authors.lastname: Huyghebaert
authors.forename: An
authors.initials: A
authors.lastname: Vermeire
authors.forename: Jean Paul
authors.initials: JP
authors.lastname: Remon
mesh_terms: D006801:Humans; D006863:Hydrogen-Ion Concentration; D007082:Ileum / Q000378:metabolism*; D016753:Interleukin-10 / Q000096:biosynthesis*; D013294:Lactococcus lactis / Q000235:genetics*; D011108:Polymers / Q000008:administration & dosage*; D011109:Polymethacrylic Acids / Q000008:administration & dosage; D011994:Recombinant Proteins / Q000096:biosynthesis; D013936:Thymidine / Q000008:administration & dosage*
chemical_list: D011108:Polymers; D011109:Polymethacrylic Acids; D011994:Recombinant Proteins; D016753:Interleukin-10; C038300:methylmethacrylate-methacrylic acid copolymer; D013936:Thymidine