Development and evaluation of innovative enteric-coated
capsules for colon-specific delivery of hydrophilic
biomaterials

J 2025

Development and evaluation of innovative enteric-coated capsules for colon-specific delivery of hydrophilic biomaterials

FÜLÖPOVÁ, Nicole; Kateřina BRÜCKNER; Jan MUSELÍK; Sylvie PAVLOKOVÁ; Aleš FRANC et al.

Základní údaje

Originální název

Development and evaluation of innovative enteric-coated capsules for colon-specific delivery of hydrophilic biomaterials

Autoři

FÜLÖPOVÁ, Nicole; Kateřina BRÜCKNER ; Jan MUSELÍK; Sylvie PAVLOKOVÁ a Aleš FRANC

Vydání

International Journal of Pharmaceutics, AMSTERDAM, ELSEVIER, 2025, 0378-5173

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

30104 Pharmacology and pharmacy

Stát vydavatele

Nizozemské království

Utajení

není předmětem státního či obchodního tajemství

Odkazy

URL

Impakt faktor

Impact factor: 5.200 v roce 2024

Organizační jednotka

Farmaceutická fakulta

DOI

https://doi.org/10.1016/j.ijpharm.2024.124991

UT WoS

001368962700001

Klíčová slova anglicky

Capsules; Coating; Immersion method; Novel approach in delayed-release dosage form with potential benefits for individual treatment; Principal component analysis

Štítky

rivok, ÚFT

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 18. 12. 2024 14:05, Mgr. Daniela Černá

Anotace

V originále

Objective: This research aims to design and evaluate an enteric-coated hard capsule dosage form for targeted delivery of biological materials, such as FMT (fecal microbiota transplant) or live microbes, to the distal parts of the GIT. The capsules are designed to be internally protected against destruction by hydrophilic filling during passage through the digestive tract. Methods: Hard gelatin capsules and DRcapsTM capsules based on HPMC and gellan were used to encapsulate a hydrophilic body temperature-liquefying gelatin hydrogel with caffeine or insoluble iron oxide mixture. Different combinations of polymers were tested for the internal (ethylcellulose, Eudragit (R) E, and polyvinyl acetate) and external (Eudragit (R) S, Acryl-EZE (R), and cellacefate) coating. The external protects against the acidic gastric environment, while the internal protects against the liquid hydrophilic filling during passage. Coated capsules were evaluated using standard disintegration and modified dissolution methods for delayed-release dosage forms. Results: Combining suitable internal (ethylcellulose 1.0 %) and external (Eudragit (R) S 20.0 %) coating of DRcapsTM capsules with the wiping and immersion method achieved colonic release times. While most coated capsules met the pharmaceutical requirements for delayed release, one combination stood out. Colonic times were indicated by the dissolution of soluble caffeine (during 120-720 min) measured by the dissolution method, and capsule rupture was indicated by the release of insoluble iron oxide (after 480 min) measured by the disintegration method. This promising result demonstrates the composition's suitability and potential to protect the content until it's released, inspiring hope for the future of colon-targeted delivery systems and its potential for the pharmaceutical and biomedical fields. Conclusion: Innovative and easy capsule coatings offer significant potential for targeted drugs, especially FMT water suspension, to the GIT, preferably the colon. The administration method is robust and not considerably affected by the quantity of internal or external coatings. It can be performed in regular laboratories without specialized individual and personalized treatment equipment, making it a practical and feasible method for drug delivery.

Citovat

FÜLÖPOVÁ, Nicole; Kateřina BRÜCKNER; Jan MUSELÍK; Sylvie PAVLOKOVÁ a Aleš FRANC. Development and evaluation of innovative enteric-coated capsules for colon-specific delivery of hydrophilic biomaterials. International Journal of Pharmaceutics. AMSTERDAM: ELSEVIER, 2025, roč. 668, Neuvedeno, s. 1-15. ISSN 0378-5173. Dostupné z: https://doi.org/10.1016/j.ijpharm.2024.124991.

@article{2461301,
   author = {Fülöpová, Nicole and Brückner, Kateřina and Muselík, Jan and Pavloková, Sylvie and Franc, Aleš},
   article_location = {AMSTERDAM},
   article_number = {Neuvedeno},
   doi = {https://doi.org/10.1016/j.ijpharm.2024.124991},
   keywords = {Capsules; Coating; Immersion method; Novel approach in delayed-release dosage form with potential benefits for individual treatment; Principal component analysis},
   language = {eng},
   issn = {0378-5173},
   journal = {International Journal of Pharmaceutics},
   title = {Development and evaluation of innovative enteric-coated capsules for colon-specific delivery of hydrophilic biomaterials},
   url = {https://pdf.sciencedirectassets.com/271189/1-s2.0-S0378517324X00198/1-s2.0-S0378517324012250/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEJT%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJGMEQCIFLykREZIkTcu1ZDZUyL8XtIDd%2FMccU4QoX0fh%2ByGzEaAiBwajj2a6F},
   volume = {668},
   year = {2025}
}

TY  - JOUR
ID  - 2461301
AU  - Fülöpová, Nicole - Brückner, Kateřina - Muselík, Jan - Pavloková, Sylvie - Franc, Aleš
PY  - 2025
TI  - Development and evaluation of innovative enteric-coated capsules for colon-specific delivery of hydrophilic biomaterials
JF  - International Journal of Pharmaceutics
VL  - 668
IS  - Neuvedeno
SP  - 1-15
EP  - 1-15
PB  - ELSEVIER
SN  - 03785173
KW  - Capsules
KW  - Coating
KW  - Immersion method
KW  - Novel approach in delayed-release dosage form with potential benefits for individual treatment
KW  - Principal component analysis
UR  - https://pdf.sciencedirectassets.com/271189/1-s2.0-S0378517324X00198/1-s2.0-S0378517324012250/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEJT%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJGMEQCIFLykREZIkTcu1ZDZUyL8XtIDd%2FMccU4QoX0fh%2ByGzEaAiBwajj2a6F
N2  - Objective: This research aims to design and evaluate an enteric-coated hard capsule dosage form for targeted delivery of biological materials, such as FMT (fecal microbiota transplant) or live microbes, to the distal parts of the GIT. The capsules are designed to be internally protected against destruction by hydrophilic filling during passage through the digestive tract. Methods: Hard gelatin capsules and DRcapsTM capsules based on HPMC and gellan were used to encapsulate a hydrophilic body temperature-liquefying gelatin hydrogel with caffeine or insoluble iron oxide mixture. Different combinations of polymers were tested for the internal (ethylcellulose, Eudragit (R) E, and polyvinyl acetate) and external (Eudragit (R) S, Acryl-EZE (R), and cellacefate) coating. The external protects against the acidic gastric environment, while the internal protects against the liquid hydrophilic filling during passage. Coated capsules were evaluated using standard disintegration and modified dissolution methods for delayed-release dosage forms. Results: Combining suitable internal (ethylcellulose 1.0 %) and external (Eudragit (R) S 20.0 %) coating of DRcapsTM capsules with the wiping and immersion method achieved colonic release times. While most coated capsules met the pharmaceutical requirements for delayed release, one combination stood out. Colonic times were indicated by the dissolution of soluble caffeine (during 120-720 min) measured by the dissolution method, and capsule rupture was indicated by the release of insoluble iron oxide (after 480 min) measured by the disintegration method. This promising result demonstrates the composition's suitability and potential to protect the content until it's released, inspiring hope for the future of colon-targeted delivery systems and its potential for the pharmaceutical and biomedical fields. Conclusion: Innovative and easy capsule coatings offer significant potential for targeted drugs, especially FMT water suspension, to the GIT, preferably the colon. The administration method is robust and not considerably affected by the quantity of internal or external coatings. It can be performed in regular laboratories without specialized individual and personalized treatment equipment, making it a practical and feasible method for drug delivery.
ER  -

FÜLÖPOVÁ, Nicole; Kateřina BRÜCKNER; Jan MUSELÍK; Sylvie PAVLOKOVÁ a Aleš FRANC. Development and evaluation of innovative enteric-coated capsules for colon-specific delivery of hydrophilic biomaterials. \textit{International Journal of Pharmaceutics}. AMSTERDAM: ELSEVIER, 2025, roč.~668, Neuvedeno, s.~1-15. ISSN~0378-5173. Dostupné z: https://doi.org/10.1016/j.ijpharm.2024.124991.

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