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

Tawfeek, Hesham M., Abdellatif, Ahmed A.H., Dennison, Thomas J., Mohammed, Afzal R., Sadiq, Younis and Saleem, Imran Y. (2017). Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets. International Journal of Pharmaceutics, in pre , pp. 80-89.

Abstract

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 ± 4.2 μg/mg) within the PGA-co-PDL microparticles. In vitro release of PGA-co-PDL-IND/Eudragit microparticles (1:1.5) showed significantly (p < 0.05, ANOVA/Tukey) lower release of IND 13.70 ± 1.6 and 56.46 ± 3.8% compared with 1:1 (89.61 ± 2.5, 80.13 ± 2.6%) and 1:0.5 (39.46 ± 0.9 & 43.38 ± 3.12) after 3 and 43 h at pH 5.5 and 6.8, respectively. The permeability and transport studies indicated IND released from PGA-co-PDL-IND/Eudragit microparticles had a lower permeability coefficient of 13.95 ± 0.68 × 10−6cm/s compared to free IND 23.06 ± 3.56 × 10−6cm/s. These results indicate the possibility of targeting anti-inflammatory drugs to the colon using FDTs containing microparticles coated with Eudragit.

Publication DOI: https://doi.org/10.1016/j.ijpharm.2017.08.069
Divisions: Life & Health Sciences > Pharmacy
Life & Health Sciences
Life & Health Sciences > Applied Health Research Group
Additional Information: © 2017, Elsevier. Licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/
Uncontrolled Keywords: colon targeting,Eudragit L100-55,fast disintegrating tablets,Indometacin,microparticles,PGA-co-PDL,spray-drying,Pharmaceutical Science
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Related URLs: http://www.scop ... tnerID=8YFLogxK (Scopus URL)
Published Date: 2017-10-05
Authors: Tawfeek, Hesham M.
Abdellatif, Ahmed A.H.
Dennison, Thomas J.
Mohammed, Afzal R. ( 0000-0002-5212-3040)
Sadiq, Younis
Saleem, Imran Y.

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