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

Hesham M. Tawfeek, Ahmed A.H. Abdellatif, Thomas J. Dennison, Afzal R. Mohammed, Younis Sadiq, Imran Y. Saleem

Research output: Contribution to journalArticle

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.

LanguageEnglish
Pages80-89
Number of pages10
JournalInternational Journal of Pharmaceutics
Volumein press
Early online date15 Aug 2017
DOIs
Publication statusPublished - 5 Oct 2017

Fingerprint

Indomethacin
Tablets
Permeability
poly(glycerol adipate-co-omega-pentadecalactone)
Eudragit L100-55
Colon
Anti-Inflammatory Agents
Caco-2 Cells
Emulsions
Inflammatory Bowel Diseases
Pharmaceutical Preparations
methylmethacrylate-methacrylic acid copolymer
Analysis of Variance
Cell Line

Bibliographical note

© 2017, Elsevier. Licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/

Keywords

  • colon targeting
  • Eudragit L100-55
  • fast disintegrating tablets
  • Indometacin
  • microparticles
  • PGA-co-PDL
  • spray-drying

Cite this

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

In: International Journal of Pharmaceutics, Vol. in press, 05.10.2017, p. 80-89.

Research output: Contribution to journalArticle

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T1 - Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets

AU - Tawfeek, Hesham M.

AU - Abdellatif, Ahmed A.H.

AU - Dennison, Thomas J.

AU - Mohammed, Afzal R.

AU - Sadiq, Younis

AU - Saleem, Imran Y.

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PY - 2017/10/5

Y1 - 2017/10/5

N2 - 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.

AB - 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.

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KW - Eudragit L100-55

KW - fast disintegrating tablets

KW - Indometacin

KW - microparticles

KW - PGA-co-PDL

KW - spray-drying

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