Colon Targeted Controlled Release System for Probiotics
Effective probiotic colonization of the colon presents distinct delivery challenges due to the harsh journey through the gastrointestinal tract. Probiotics must navigate gastric acid exposure (pH 1.5-3.5) and enzymatic degradation in the upper GI tract, which typically results in viability losses exceeding 90% before reaching the colon. Furthermore, residence time in the target colonization zone averages only 12-24 hours, necessitating both protection during transit and efficient attachment mechanisms once delivered.
The fundamental challenge lies in developing delivery systems that protect probiotic viability through the upper GI tract while enabling precise release and colonization specifically in the colon microenvironment.
This page brings together solutions from recent research—including pH-dependent enteric coating systems, microbial-triggered release mechanisms, chitosan-iron protective encapsulation, and mucoadhesive barrier technologies. These and other approaches address the practical requirements for maintaining probiotic stability during transit while maximizing colonization potential through targeted colonic delivery.
1. Ingestible Devices with Trigger-Activated Drug Reservoirs and Piercer-Enabled Gas Ejection for Gastrointestinal Tract Delivery
BIORA THERAPEUTICS INC, 2025
Ingestible devices for targeted delivery of therapeutics to specific regions of the gastrointestinal tract. The devices can deliver drugs trans-epithelially, epithelially, or topically to the GI tract. The devices contain a reservoir of drug that is released when a trigger mechanism dissolves or erodes in the desired location. This allows targeted drug delivery to avoid systemic absorption. The devices can also have a piercer to access a gas container for forceful drug ejection. The devices are swallowed and travel through the GI tract to deliver drugs at specific locations.
2. Dress me an outfit: advanced probiotics hybrid systems for intelligent IBD therapy
Yonglu Li, Yadi Wang, Yapeng Li - Informa UK Limited, 2025
Inflammation bowel disease (IBD) has emerged as a public health challenge worldwide; with high incidence and rapid prevalence, it has troubled billions of people and further induced multitudinous systemic complications. Recent decade has witnessed the vigorous application of food-borne probiotics for IBD therapy; however, the complicated and changeable environments of digestive tract have forced probiotics to face multiple in vivo pressures, consequently causing unsatisfied prophylactic or therapeutic efficacy attributed to off-targeted arrival, damaged viability, insufficient colonization efficiency, etc. Fortunately, arisen hybrid technology has provided versatile breakthroughs for the targeted transplantation of probiotics. By ingeniously modifying probiotics to form probiotics hybrid systems (PHS), the biological behaviors of probiotics in vivo could be mediated, the interactions between probiotics with intestinal components can be facilitated, and diverse advanced probiotic-based therapies for IBD challenge can be developed, which attribute to the intelligent response to microen... Read More
3. Intestinal Tissue Penetrating Members with Sharp Beveled Edge and Central Longitudinal Axis
ALMA THERAPEUTICS LTD, 2024
Intestinal tissue penetrating members with enhanced penetration capability for targeted drug delivery. The members feature a body portion with a central longitudinal axis and a tissue penetrating end with a sharp beveled edge, specifically designed to penetrate intestinal wall layers through a single, controlled penetration motion. The edge maintains a taut cutting zone, allowing precise tissue penetration while minimizing tissue damage. The members can be mounted on a delivery device, such as an inflatable patch, for targeted delivery through the intestinal wall.
4. Carbohydrate polymer-based carriers for colon targeted delivery of probiotics
Wanli Zhang, Alireza Sadeghi, Aslı Can Karaça - Informa UK Limited, 2024
AbstractProbiotics (PRO) have been recognized for their significant role in promoting human health, particularly in relation to colon-related diseases. The effective delivery of PRO to the colon is a fascinating area of research. Among various delivery materials, carbohydrates have shown great potential as colon-targeted delivery (CTD) carriers for PRO. This review explores the connection between probiotics and colonic diseases, delving into their underlying mechanisms of action. Furthermore, it discusses current strategies for the targeted delivery of active substances to the colon. Unlike other reviews, this work specifically focuses on the utilization of carbohydrates, such as alginate, chitosan, pectin, and other carbohydrates, for probiotic colon-targeted delivery applications. Carbohydrates can undergo hydrolysis at the colonic site, allowing their oligosaccharides to function as prebiotics or as direct functional polysaccharides with beneficial effects. Furthermore, the development of multilayer self-assembled coatings using different carbohydrates enables the creation of enha... Read More
5. Intracellularly Gelated Macrophages Loaded with Probiotics for Therapy of Colitis
Siyao Gu, Xiaona Zhao, Fang Wan - American Chemical Society (ACS), 2024
Probiotics therapy has garnered significant attention in the treatment of inflammatory bowel disease (IBD). However, a large number of oral administrated probiotics are inactivated after passing through the gastric acid environment, and their ability to colonize in the intestine is also weak. Herein, this study develops a novel probiotics formulation (GM-EcN) by incorporating
6. Fermented Soymilk with Probiotic Lactobacilli and Bifidobacterium Strains Ameliorates Dextran-Sulfate-Sodium-Induced Colitis in Rats
Ashwag Jaman Al Zahrani, Amal Bakr Shori, Effat Al-Judaibi - MDPI AG, 2024
: Current treatments for inflammatory bowel disease (IBD) are relatively futile and the extended use of drugs may reduce effectiveness. Several probiotic strains have shown promise in relieving/treating IBD symptoms.
7. 3D-Printed Oral Dosage Form with pH-Sensitive Enteric Member for Targeted Colonic Drug Release
TRIASTEK INC, 2024
Oral drug dosage forms configured to release a drug at a desired location in the colon of an individual, comprising a drug component and a delay component. The delay component prevents drug release until the dosage form reaches the colon, and comprises a pH-based enteric member that erodes at a predetermined pH value. The dosage form can be designed and manufactured using 3D printing, and can be used to treat a range of conditions including gastrointestinal disorders, CNS disorders, and cardiovascular disease.
8. Investigating the effects of combined treatment of mesalazine with Lactobacillus casei in the experimental model of ulcerative colitis
Shabnam Bahrami, Nahid Babaei, Hadi Esmaeili Gouvarchin Ghaleh - Frontiers Media SA, 2024
Ulcerative colitis (UC), a common gastrointestinal disorder in affluent nations, involves chronic intestinal mucosal inflammation. This research investigated the effects of combined probiotic treatment of
9. Probiotic <i>Lactiplantibacillus plantarum</i> subsp. <i>plantarum</i> Dad-13 Alleviates 2,4,6-Trinitrobenzene Sulfonic Acid-Induced Colitis Through Short-Chain Fatty Acid Production and Inflammatory Cytokine Regulation
Rimba Bunga Pertiwi, Yosinta Christie Setiabudi, Yunika Mayangsari - The Korean Society of Food Science and Nutrition, 2024
The development of inflammatory bowel disease (IBD) is closely linked to inflammatory damage and dysbiosis. Recently, probiotics are being increasingly used to improve intestinal health. Probiotic-based therapies can prevent IBD by restoring the balance of gastrointestinal microbiota, reducing gut inflammation, and increasing the concentration of short-chain fatty acids (SCFAs). The present study aimed to investigate the protective effects of
10. Lactic Acid Bacterial Fermentation of Esterified Agave Fructans in Simulated Physicochemical Colon Conditions for Local Delivery of Encapsulated Drugs
Carmen Miramontes-Corona, Abraham Cetina-Corona, María Esther Macías-Rodríguez - MDPI AG, 2024
Understanding drug release in the colon is fundamental to developing efficient treatments for colon-related diseases, while unraveling the relationship between the colonic microbiota and excipients is crucial to unveiling the effect of biomaterials on the release of drugs. In this contribution, the bio-release of ibuprofen (encapsulated in acetylated and palmitoylated agave fructans) was evaluated by fermentation with lactic acid bacteria in simulated physicochemical (pH and temperature) colon conditions. It was observed that the size of the acyl chain (1 in acetyl and 15 in palmitoyl) was critical both in the growth of the microorganisms and in the release of the drug. For example, both the bacterial growth and the release of ibuprofen were more favored with acetylated fructan microspheres. Among the microorganisms evaluated, Bifidobacterium adolescentis and Lactobacillus brevis showed great potential as probiotics useful to release drugs from modified fructans. The production of short-chain fatty acids (lactic, acetic, and propionic acids) in the course of fermentations was also de... Read More
11. Oral Intestinal Drug Delivery Formulation with Microbial-Sensitive Inner Coating and Enteric Outer Coating
NBI BIOSCIENCES PVT LTD, 2024
Microbial-triggered oral intestinal drug delivery formulation that targets the small and large intestine for precise drug delivery. The formulation comprises an outer enteric coating, an inner coating, and a central core, which work together to prevent premature drug release in the upper GI tract and ensure delivery to the colon. The inner coating contains a microbial-sensitive component that triggers drug release in response to the natural microbial flora of the intestine.
12. Engineering a Novel Probiotic Toolkit in <i>Escherichia coli</i> <i>Nissle 1917</i> for Sensing and Mitigating Gut Inflammatory Diseases
Nathalie Weibel, Martina Curcio, Atilla Schreiber - American Chemical Society (ACS), 2024
Inflammatory bowel disease (IBD) is characterized by chronic intestinal inflammation with no cure and limited treatment options that often have systemic side effects. In this study, we developed a target-specific system to potentially treat IBD by engineering the probiotic bacterium
13. Lacticaseibacillus casei IB1 Alleviates DSS-Induced Inflammatory Bowel Disease by Regulating the Microbiota and Restoring the Intestinal Epithelial Barrier
Jianlong Lao, NULL AUTHOR_ID, NULL AUTHOR_ID - MDPI AG, 2024
Inflammatory bowel disease (IBD) is becoming an increasingly serious health problem in humans and animals. Probiotics can inhibit the development of IBD. Due to the specificity of the strains, the function and mechanism of action of different strains are still unclear. Here, a DSS-induced colitis mouse model was utilized to investigate the ability and mechanism by which
14. Breaking barriers: bacterial-microalgae symbiotic systems as a probiotic delivery system
Hui Huang, Xiaoyang Liu, Yutong Lang - Springer Science and Business Media LLC, 2024
Abstract The gut microbiota is one of the essential contributors of the pathogenesis and progress of inflammatory bowel disease (IBD). Compared with first-line drug therapy, probiotic supplementation has emerged as a viable and secure therapeutic approach for managing IBD through the regulation of both the immune system and gut microbiota. Nevertheless, the efficacy of oral probiotic supplements is hindered by their susceptibility to the gastrointestinal barrier, leading to diminished bioavailability and restricted intestinal colonization. Here, we developed a bacteria-microalgae symbiosis system (EcN-SP) for targeted intestinal delivery of probiotics and highly effective treatment of colitis. The utilization of mircroalge Spirulina platensis (SP) as a natural carrier for the probiotic Escherichia coli Nissle 1917 (EcN) demonstrated potential benefits in promoting EcN proliferation, facilitating effective intestinal delivery and colonization. The alterations in the binding affinity of EcN-SP within the gastrointestinal environment, coupled with the distinctive structural properties o... Read More
15. Capsule with Modified-Release Coating and Hydrophilic Isolating Layer for Intestinal Drug Delivery
JIANGSU HENGRUI PHARMACEUTICALS CO LTD, 2024
A capsule for targeted intestinal drug delivery, comprising a modified-release coating and an isolating layer between the coating and the capsule shell. The isolating layer contains a hydrophilic molecule, such as sucrose, which prevents premature release of the drug and ensures effective delivery to the intestinal tract. The capsule is filled with a sustained-release formulation containing a corticosteroid, such as budesonide, and hydroxypropyl methylcellulose, with a weight ratio of at least 2.5:1. The modified-release coating is an enteric coating comprising Eudragit L100 and triethyl citrate.
16. Pellet-Based Formulation with pH-Dependent and pH-Independent Coatings for Colon Delivery
ADD ADVANCED DRUG DELIVERY TECHNOLOGIES LTD, 2024
Delayed release pharmaceutical formulation for colon delivery of water-soluble active pharmaceutical ingredients, comprising pellets with a core and a layered coating. The core contains the API, while the coating consists of a pH-dependent release layer and a pH-independent sustained release layer. The pH-dependent layer releases the API above pH 7.0, while the pH-independent layer provides sustained release. The formulation enables targeted and modified release of the API in the colon, particularly for APIs like metformin hydrochloride.
17. Pharmaceutical Composition with Multi-Layered Core for Colon-Targeted Oral Delivery
AXIAL THERAPEUTICS INC, 2024
A pharmaceutical composition for oral delivery of therapeutic agents to the colon, comprising a core of therapeutic agent surrounded by multiple layers that control release to specifically target the descending colon. The composition includes a pH-sensitive layer, a hydrolyzed zein-derived material, and a polysaccharide layer, which can be applied in various combinations to achieve delayed-burst release in the colon. The composition is particularly useful for treating conditions such as autism spectrum disorder, chronic kidney disease, and uremic symptoms, by delivering therapeutic agents such as adsorbents and sequestrants directly to the colon.
18. Colon Specific and Targeted Drug Delivery System (CDDS): A Review
Nimesh Agrawal, Navneet Kumar Verma, Saumya Srivastava - SASPR Edu International Pvt. Ltd, 2024
In the recent year colonic drug delivery is important for delivery of drug for the treatment of local disease. Targeted drug delivery into the colon is highly desirable for local treatment of a variety of bowel diseases such as ulcerative colitis, Crohns disease, amoebiosis, colonic cancer, local treatment of colonic pathologies, and systemic delivery of protein and peptide drugs. This article gives overview on different approaches of colon targeted drug delivery system such as pH sensitive polymer coated drug delivery to colon, time Controlled release drug delivery to Colon microbially triggered systems, prodrug approach to drug delivery to colon it also consist of recent approaches of colon targeted drug delivery such as pressure controlled drug-Delivery Systems, Novel Colon Targeted Delivery System (CODESTM), Osmotic Controlled Drug Delivery (ORDS-CT).
19. Current Update of Clinical Therapeutic Strategies for Colon-Targeted Delivery Systems
- Universitas Indonesia, 2024
Oral colon-targeted drug delivery systems represent a significant advancement offering both systemic and local therapeutic effects for a range of intestinal diseases, including irritable bowel syndrome, inflammatory bowel disease, colonic bacterial infections, and colorectal cancer. These systems facilitate the delivery of both small molecules and macromolecular compounds such as peptides, proteins, antibodies, oligonucleotides, RNA, and probiotics. This review provides an up-to-date exploration of the critical factors crucial for the effective design and development of drug delivery systems targeting the colon. The chosen strategy takes into account various aspects of colon physiology that influences the profile of drug release, absorption, dissolution, and stability in the colon, including pH, retention time, presence of enzymes, pressure, presence of reactive oxygen species due to inflammation, and specific receptors. Site-targeted drug release allows for high concentrations in the colon while minimizing systemic adverse effects by reducing or preventing drug absorption in the sma... Read More
20. Personalized probiotic strategy considering bowel habits: impacts on gut microbiota composition and alleviation of gastrointestinal symptoms via Consti-Biome and Sensi-Biome
Ui-Gi Min, Yoo-Jeong Jin, You Jin Jang - Frontiers Media SA, 2024
Personalized probiotic regimens, taking into account individual characteristics such as stool patterns, have the potential to alleviate gastrointestinal disorders and improve gut health while avoiding the variability exhibited among individuals by conventional probiotics. This study aimed to explore the efficacy of personalized probiotic interventions in managing distinct stool patterns (constipation and diarrhea) by investigating their impact on the gut microbiome and gastrointestinal symptoms using a prospective, randomized, double-blind, placebo-controlled clinical trial design. This research leverages the multi-strain probiotic formulas, Consti-Biome and Sensi-Biome, which have previously demonstrated efficacy in alleviating constipation and diarrhea symptoms, respectively. Improvement in clinical symptoms improvement and compositional changes in the gut microbiome were analyzed in participants with predominant constipation or diarrhea symptoms. Results indicate that tailored probiotics could improve constipation and diarrhea by promoting
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