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.

Basic information

Original name

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

Authors

FÜLÖPOVÁ, Nicole (703 Slovakia, belonging to the institution); Kateřina BRÜCKNER (203 Czech Republic, belonging to the institution); Jan MUSELÍK (203 Czech Republic, belonging to the institution); Sylvie PAVLOKOVÁ (203 Czech Republic, belonging to the institution) and Aleš FRANC (203 Czech Republic, belonging to the institution)

Edition

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

Other information

Language

English

Type of outcome

Article in a journal

Field of Study

30104 Pharmacology and pharmacy

Country of publisher

Netherlands

Confidentiality degree

is not subject to a state or trade secret

References:

Impact factor

Impact factor: 5.300 in 2023

Organization unit

Faculty of Pharmacy

UT WoS

001368962700001

Keywords in English

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

Tags

Tags

International impact, Reviewed
Changed: 18/12/2024 14:05, Mgr. Daniela Černá

Abstract

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.