Fülöpová Nicole, Brückner Kateřina, Muselík Jan, Pavloková Sylvie, Franc Aleš
Department of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, Brno 612 00, Czech Republic.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, Brno 612 00, Czech Republic.
Int J Pharm. 2025 Jan 5;668:124991. doi: 10.1016/j.ijpharm.2024.124991. Epub 2024 Nov 22.
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.
Hard gelatin capsules and DRcapscapsules 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® E, and polyvinyl acetate) and external (Eudragit® S, Acryl-EZE®, 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.
Combining suitable internal (ethylcellulose 1.0 %) and external (Eudragit® S 20.0 %) coating of DRcaps 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.
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.
本研究旨在设计并评估一种肠溶硬胶囊剂型，用于将生物材料（如粪便微生物群移植（FMT）或活微生物）靶向递送至胃肠道远端。这些胶囊的设计目的是在通过消化道的过程中，内部受到保护，防止亲水性填充物将其破坏。
使用硬明胶胶囊以及基于羟丙甲纤维素（HPMC）和结冷胶的DRcaps胶囊，来封装含有咖啡因或不溶性氧化铁混合物的亲水性体温液化明胶水凝胶。对内部包衣（乙基纤维素、Eudragit® E和聚醋酸乙烯酯）和外部包衣（Eudragit® S、Acryl-EZE®和醋酸纤维素）的不同聚合物组合进行了测试。外部包衣可防止酸性胃环境的影响，而内部包衣可在通过过程中防止液体亲水性填充物的破坏。使用标准崩解和改良溶出方法对包衣胶囊进行延迟释放剂型的评估。
通过擦拭和浸泡法，将合适的内部（1.0%乙基纤维素）和外部（20.0% Eudragit® S）包衣应用于DRcaps胶囊，实现了结肠释放时间。虽然大多数包衣胶囊符合延迟释放的药学要求，但有一种组合尤为突出。通过溶出法测定可溶性咖啡因的溶解情况（120 - 720分钟内）来表明结肠释放时间，通过崩解法测定不溶性氧化铁的释放情况（480分钟后）来表明胶囊破裂。这一有前景的结果证明了该组合物在保护内容物直至释放方面的适用性和潜力，为结肠靶向递送系统的未来及其在制药和生物医学领域的潜力带来了希望。
创新且简便的胶囊包衣为将靶向药物，尤其是FMT水悬浮液，递送至胃肠道，优选结肠，提供了巨大潜力。给药方法稳健，不受内部或外部包衣量的显著影响。它可以在常规实验室中进行，无需专门的个体化和个性化治疗设备，使其成为一种实用且可行的药物递送方法。
