Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets

• Published in: International journal of pharmaceutics 2017-10, Vol.531 (1), p.80-89
• Main Authors: Tawfeek, Hesham M., Abdellatif, Ahmed A.H., Dennison, Thomas J., Mohammed, Afzal R., Sadiq, Younis, Saleem, Imran Y.
• Format: Article
• Language: English
• Subjects: Acrylic Resins - chemistry; Caco-2 Cells; Colon targeting; Drug Delivery Systems; Eudragit L100-55; Fast disintegrating tablets; Humans; Hydrogen-Ion Concentration; Indometacin; Indomethacin - administration & dosage; Microparticles; PGA-co-PDL; Polyesters - chemistry; Polymethacrylic Acids; Spray-drying; Tablets
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2017.08.069

[Display omitted] The aim of this work was to investigate the efficient targeting and delivery of indometacin (IND), as a model anti-inflammatory drug to the colon for treatment of inflammatory bowel disease. We prepared fast disintegrating tablets (FDT) containing IND encapsulated within poly(glycerol-adipate-co-ɷ-pentadecalactone), PGA-co-PDL, microparticles and coated with Eudragit L100-55 at different ratios (1:1.5, 1:1, 1:0.5). Microparticles encapsulated with IND were prepared using an o/w single emulsion solvent evaporation technique and coated with Eudragit L-100-55 via spray drying. The produced coated microparticles (PGA-co-PDL-IND/Eudragit) were formulated into optimised FTD using a single station press. The loading, in vitro release, permeability and transport of IND from PGA-co-PDL-IND/Eudragit microparticles was studied in Caco-2 cell lines. IND was efficiently encapsulated (570.15±4.2μg/mg) within the PGA-co-PDL microparticles. In vitro release of PGA-co-PDL-IND/Eudragit microparticles (1:1.5) showed significantly (p