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

doi:10.1016/j.ijpharm.2017.08.069

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

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	80-89
Number of pages	10
Journal	International Journal of Pharmaceutics
Volume	531
Issue number	1
Early online date	15 Aug 2017
DOIs	https://doi.org/10.1016/j.ijpharm.2017.08.069
Publication status	Published - 5 Oct 2017

Bibliographical note

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

Funding: Dr Hesham Tawfeek would like to thank the Egyptian Ministry of Higher Education for the financial support.

Keywords

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

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10.1016/j.ijpharm.2017.08.069

Colonic delivery of indometacin loaded PGA-co-PDL microparticles
© 2017, Elsevier. Licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/
Accepted author manuscript, 926 KBLicence: CC BY-NC-ND 3.0

Cite this

@article{20ea6ded9fc24f159ac32fb6c392dc8f,

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

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.",

keywords = "colon targeting, Eudragit L100-55, fast disintegrating tablets, Indometacin, microparticles, PGA-co-PDL, spray-drying",

author = "Tawfeek, {Hesham M.} and Abdellatif, {Ahmed A.H.} and Dennison, {Thomas J.} and Mohammed, {Afzal R.} and Younis Sadiq and Saleem, {Imran Y.}",

note = "{\textcopyright} 2017, Elsevier. Licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/ Funding: Dr Hesham Tawfeek would like to thank the Egyptian Ministry of Higher Education for the financial support.",

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doi = "10.1016/j.ijpharm.2017.08.069",

language = "English",

volume = "531",

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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.

N1 - © 2017, Elsevier. Licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/ Funding: Dr Hesham Tawfeek would like to thank the Egyptian Ministry of Higher Education for the financial support.

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.

KW - colon targeting

KW - Eudragit L100-55

KW - fast disintegrating tablets

KW - Indometacin

KW - microparticles

KW - PGA-co-PDL

KW - spray-drying

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DO - 10.1016/j.ijpharm.2017.08.069

M3 - Article

AN - SCOPUS:85027719796

SN - 0378-5173

VL - 531

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EP - 89

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 1

ER -

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

Abstract

Bibliographical note

Keywords

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