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
21. Chitosan-Iron Coated Synbiotic Microcapsule with Gastric Acid Resistance and Intestinal Release Mechanism
SINO-AGRI PET NUTRITION RESEARCH INSTITUTE, 2024
A chitosan-Fe coating-based synbiotic microcapsule with gastric acid resistance and intestinal targeted release, prepared by encapsulating a mixed probiotic-prebiotic core material with a chitosan-Fe solution and freeze-drying protective agent. The microcapsule exhibits improved probiotic survival and intestinal targeting, overcoming limitations of conventional microencapsulation methods.
22. Microfluidics-Derived Microparticles with Prebiotics and Probiotics for Enhanced In Situ Colonization and Immunoregulation of Colitis
Yi Yin, Zhun Li, Hengfei Gao - American Chemical Society (ACS), 2024
Oral administration of probiotics orchestrates the balance between intestinal microbes and the immune response. However, effective delivery and in situ colonization are limited by the harsh environment of the gastrointestinal tract. Herein, we provide a microfluidics-derived encapsulation strategy to address this problem. A novel synergistic delivery system composed of EcN Nissle 1917 and prebiotics, including alginate sodium and inulin gel, for treating inflammatory bowel disease and colitis-associated colorectal cancer is proposed. We demonstrated that EcN@AN microparticles yielded promising gastrointestinal resistance for on-demand probiotic delivery and colon-retentive capability. EcN@AN microparticles efficiently ameliorated intestinal inflammation and modulated the gut microbiome in experimental colitis. Moreover, the prebiotic composition of EcN@AN enhanced the fermentation of relative short-chain fatty acid metabolites, a kind of postbiotics, to exert anti-inflammatory and tumor-suppressive effects in murine models. This microfluidcis-based approach for the coordinated delive... Read More
23. Advanced Drug Delivery Approaches Containing Synbiotics
Popat Kumbhar, Kaustubh Kolekar, Rajnandini Patil - Springer Nature Singapore, 2024
Synbiotics have shown various beneficial effects in inflammatory bowel diseases, irritable bowel syndrome, infectious disorders, and diarrheal illnesses. However, the delivery of probiotics to the host intestine is challenging owing to the poor survivability and viability of probiotic bacteria during the gastric transit, and poor stability at the highly acidic pH of the stomach. The oral delivery of probiotics in combination with prebiotics can achieve the targeted delivery of probiotics toward the intestine. The deliveries of synbiotics through suitable particulate carriers can also be useful to improve the encapsulation efficiency, viability, stability, and performance of probiotics. In addition, these particulate carriers also help to control the release of probiotics at the target site (intestine). This chapter discusses the synbiotics and various particulate carriers in synbiotics delivery along with multiple case studies. Further, the synbiotics in clinical trials and regulatory aspects of synbiotics are also highlighted.
24. Recent advances in probiotics oral delivery systems targeting the inflammatory bowel disease: Types, mechanisms and perspectives
Yaxin Yin, Xiaoqun Zeng, Zhen Wu - Tsinghua University Press, 2024
Inflammatory bowel disease (IBD) influences several million people around the globe, with a high prevalence in North America and Europe. Results from the studies about host-gut microbial interactions demonstrated that gut microbiota plays a critical role in the progression of IBD, and probiotics can significantly improve microflora dysbiosis and inflammatory response caused by intestinal pathogens. However, several limitations existed for the probiotics delivered to the intestine in the free form (non-encapsulated), such as low pH and diverse digestive enzymes in the gastrointestinal tract, etc. To overcome the problems, several probiotic delivery systems were established and verified with effects. Here, the types and applications of probiotics in animal models and clinical studies are firstly reviewed in this paper. Subsequently, various types of probiotic delivery systems are elaborated, containing the well-known microcapsules and hydrogel delivery systems, and the engineered probiotic delivery systems are also introduced. Furthermore, mechanism of action associated with probiotics... Read More
25. Surviving process and transit: Controlled freeze drying, storage and enteric coated capsules for targeted delivery of probiotic Lactobacillus acidophilus
Mansa Fredua‐Agyeman - Elsevier BV, 2024
Viability loss of probiotics often occur during processing, storage and gastrointestinal transit. In this study, the viability of freeze-dried
26. Microfluidic-based multifunctional microspheres for enhanced oral co-delivery of probiotics and postbiotics
Xinyuan Yang, Weimin Nie, Chong Wang - Elsevier BV, 2024
Probiotic-based therapies have shown great potential in the prevention and treatment of many diseases by positively regulating intestinal flora homeostasis. However, the efficacy of oral probiotics is severely limited due to the loss of bioactivity, short intestinal retention time, and insufficient therapeutic effect. Here, based on droplet microfluidics, we developed a hydrogel microsphere with colonic targeting and mucoadhesive capabilities as a multifunctional delivery platform, which can be used for co-delivery of probiotics (Escherichia coli Nissle 1917, EcN) and auxiliary molecules (indole-3-propionic acid, IPA), achieving synergistic therapeutic effects. In vivo studies shown that the integrated multifunctional microspheres can significantly reduce intestinal inflammation, repair intestinal barrier function, enhance probiotic colonization in the intestine, and modulate disordered intestinal flora, demonstrating enhanced therapeutic effects in a mouse model of colitis. This work reveals that microfluidic-based smart droplet microspheres can provide a versatile platform for adva... Read More
27. He who controls Clostridia and Bacteroidia controls the gut microbiome: The concept of targeted probiotics to restore the balance of keystone taxa in irritable bowel syndrome
Juris Pokrotnieks, С. И. Ситкин - Wiley, 2024
Abstract This article describes the concept of probiotics for patients with irritable bowel syndrome to target functionally active bacteria predominantly belonging to the Clostridia and Bacteroidia, which play a key role in maintaining the balance of the gut microbiota.
28. Retrospective subgroup analysis of fecal microbiota, live-jslm (REBYOTA<sup>®</sup>) administered by colonoscopy under enforcement discretion for the prevention of recurrent <i>Clostridioides difficile</i> infection
W Knapple, David Yoho, Alexander Sheh - SAGE Publications, 2024
Background: Fecal microbiota, live-jslm (RBL; REBYOTA ), is the first Food and Drug Administration (FDA)-approved, single-dose, rectally administered, microbiota-based live biotherapeutic product for preventing Clostridioides difficile infection (CDI) recurrence. Alternative routes of administration are of clinical interest. Objectives: Evaluate the safety and efficacy of RBL administration via colonoscopy. Design: Retrospective analysis of electronic medical records of participants administered RBL via colonoscopy under FDA enforcement discretion. Methods: The number of participants with treatment and/or procedure-emergent adverse events (TEAEs) was evaluated. Treatment success and sustained clinical response, defined as the absence of CDI recurrence within 8 weeks and 6 months, respectively, were evaluated. Results: TEAEs were experienced by 75% (6/8) of participants; most were mild to moderate in severity, and none due to RBL or its administration. Most participants had treatment success (80%; 8/10); 75% (6/8) had sustained clinical response. Conclusion: Real-world safety and ef... Read More
29. In Vitro Development of Enteric-Coated Tablets of the Probiotic Lactobacillus fermentum LF-G89: A Possible Approach to Intestinal Colonization
Paola Spínello, Pâmela do Nascimento, Verônica Cristina da Silveira - Bentham Science Publishers Ltd., 2024
Probiotics must be able to withstand the demanding environment of the gastrointestinal system to adhere to the intestinal epithelium, promoting health benefits. The use of probiotics can prevent or attenuate the effects of dysbiosis that have a deleterious effect on health, promoting anti-inflammatory, immunomodulatory, and antioxidant effects.
30. Colon Targeted Delivery Dosage Forms for Probiotics: A Review
Gede Anjasmara, Pietradewi Hartrianti, Raditya Iswandana - Universitas Indonesia, 2023
Encapsulation was a promising method for protecting probiotics from extreme conditions during their passage through the gastrointestinal tract and delivering probiotics to specific sites in the colon for colonization. Various dosage forms have been used in recent years to encapsulate probiotics to maintain cell viability during processing, storage, and through the digestive tract to provide health benefits. However, research related to the encapsulation of probiotics as the dosage forms for colon-targeted delivery systems was still quite limited to conventional dosage forms due to the sensitivity of probiotics to extreme conditions during the process. This review focuses on various types of dosage forms that are used in colon-targeted delivery systems for commonly used probiotic bacteria. In this review, we discussed the limitations of the current dosage forms used in probiotic encapsulation, along with the latest advancements in colon-targeted delivery systems for probiotic products. This review also covers future perspectives on the potential dosage forms that can effectively maint... Read More
31. 10. LITERATURE REVIEW OF RESEARCH AND DEVELOPMENT OF PROBIOTIC TABLETS
Ngo Nguyen Quynh Anh, Đàm Thanh Xuân, Nguyen Ngoc Chien - Institute of Community Health, 2023
Probiotics are gaining increasing attention due to their significant benefits to the host. Despite their potential advantages, probiotic dosage forms have not been extensively studied, primarily because of their poor survival through the gastrointestinal tract. Probiotic tablets emerge as a promising delivery system utilized in nutritional products to supplement the natural intestinal flora. These tablets possess the capability to deliver live, functional bacteria in sufficiently large quantities, ensuring effectiveness, and providing protection against the harsh conditions of the gastrointestinal and biliary tract environment, thereby ensuring in vivo protection and maintaining viability during preparation. Various adverse effects that impact the effectiveness of probiotics are associated with preparation methods and user factors. This review primarily focuses on probiotic tablets, delving into factors influencing the existence of microorganisms and the development of formulations for probiotic tablets.
32. Compositions with Mucoadhesive Barrier Layer for Directional Control of Active Agent Release
ALTRIXBIO INC, 2023
Therapeutic compositions for targeted delivery of active agents through the gastrointestinal tract, featuring a mucoadhesive agent that selectively forms a barrier layer on the active agent while preventing release in the opposite direction. The compositions can be formulated as drug delivery systems for specific therapeutic applications, including targeted delivery to the GI tract.
33. Microcapsule Powder with Thermally Stable Enzyme-Degradable Coating for Intestinal Release
HOBOOMLIFE BIO-TECHNOLOGY CO LTD, 2023
Microcapsule powder for oral delivery of sensitive compounds, comprising a core material coated with a thermally stable capsule material that resists gastric acid and proteases but degrades in intestinal enzymes, ensuring controlled release of the core material in the intestine.
34. Bacteriocin-Producing Lactiplantibacillus plantarum YRL45 Enhances Intestinal Immunity and Regulates Gut Microbiota in Mice
Yushan Bu, Yisuo Liu, Tai Zhang - MDPI AG, 2023
Bacteriocins production is one of important beneficial characteristics of probiotics, which has antibacterial property against intestinal pathogens and is helpful for regulating intestinal flora. To investigate the impact of bacteriocin-producing probiotics on gut microecology, bacteriocin-producing Lactiplantibacillus plantarum YRL45 was orally administered to mice. The results revealed that it promoted the release of cytokines and improved the phagocytic activity of peritoneal macrophages to activate the immune regulation system. L. plantarum YRL45 was conducive to maintaining the morphology of colon tissue without inflammation and increasing the ratio of villus height to crypt depth in the ileum. The gene expression levels of Muc2, ZO-1 and JAM-1 were significantly up-regulated in the ileum and colon, and the gene expression of Cramp presented an upward trend with L. plantarum YRL45 intervention. Moreover, L. plantarum YRL45 remarkably enhanced the levels of immunoglobulins sIgA, IgA and IgG in the intestine of mice. The 16S rRNA gene analysis suggested that L. plantarum YRL45 adm... Read More
35. Gastric Retention Dosage Form with Fluid-Absorptive Core and Semi-Permeable Viscoelastic Surface Layer
ARON H BLAESI, 2023
A gastric retention dosage form comprising a drug-containing solid with a fluid-absorptive core and a mechanically strengthening, semi-permeable surface layer. Upon exposure to physiological fluid, the core expands with fluid absorption, transitioning to a viscous or semi-solid mass, while the surface layer forms a semi-permeable, viscoelastic membrane that expands due to internal pressure generated by osmotic fluid flow. The dosage form maintains its expanded state for an extended period, enabling controlled drug release.
36. Pharmaceutical Compositions with Enteric-Coated Dosage Forms for Enteroendocrine Cell Stimulation
APHAIA PHARMA IP AG, 2023
Pharmaceutical compositions and articles comprising multiple dosage forms each comprising a core and an enteric coating, wherein the core comprises at least one compound stimulating enteroendocrine cells to release at least one enterokine, and the size of the dosage forms, with respect to the largest dimension of the dosage forms, provides for entry of the dosage forms into the intestine of a subject independent of gastric emptying mechanisms, and wherein the composition further comprises one or more gelling agents.
37. Softgel Capsules with pH-Dependent Gelatin-Dextrose-Pectin Shell Composition for Colonic Delivery
SCHERER TECHNOLOGIES LLC R P, 2023
Delayed release softgel capsules with pH-dependent shell compositions that enable targeted colonic delivery without the need for pH-dependent coatings or conventional pH-dependent polymers. The shell composition comprises gelatin, dextrose, and pectin, which interact to create a pH-dependent barrier that protects the fill material from gastric conditions while allowing controlled release in the colon. The composition can be optimized for specific pH dissolution profiles and can be manufactured using conventional softgel processes.
38. Enteric Capsule with Mucosa-Penetrating Drug-Containing Particles for Intestinal Delivery
JANSSEN BIOTECH INC, 2023
A drug delivery system for localized treatment of gastrointestinal diseases, comprising an enteric capsule containing a plurality of drug-containing particles that penetrate the intestinal mucosa. The particles have a matrix body and active pharmaceutical ingredient distributed within, and are configured to adsorb into and/or embed within the intestinal lining. The enteric capsule is designed to release the particles in the small or large intestine, where they can provide targeted therapy to diseased tissue.
39. Evaluation of the effectiveness of personalised therapy for the patients with irritable bowel syndrome
Е. И. Ермоленко, С. И. Ситкин, Timur Vakhitov - Walter de Gruyter GmbH, 2023
Intestinal microbiota correction in the therapy of irritable bowel syndrome (IBS) is an important medical problem. We conducted a laboratory and pilot clinical trial to investigate the effect of autoprobiotic bacteria, indigenous bifidobacteria and enterococci isolated from faeces and grown on artificial media to use as personified food additives in IBS treatment. Convincing evidence of the clinical efficacy of autoprobiotic was demonstrated by the disappearance of dyspeptic symptoms. The microbiome of patients with IBS was compared to a group of healthy volunteers and changes in the microbiome after autoprobiotic use were detected by quantitative polymerase chain reaction and 16S rRNA metagenome analysis. The possibility of reducing opportunistic microorganisms in the treatment of IBS with autoprobiotics has been convincingly proven. The quantitative content of enterococci in the intestinal microbiota was higher in IBS patients than in healthy volunteers and increased after therapy. An increase in the relative abundance of genera Coprococcus, Blautia and a decrease in the relative a... Read More
40. Encapsulation Particles with Controlled Release Kinetics and Variable Delivery Profiles
NULIXIR INC, 2023
Manufacturing small particles that mask the flavor of the encapsulated ingredients, control the release kinetics of the encapsulated ingredients after consumption, control the delivery location (e.g., organ) of the encapsulated ingredients, stabilize the encapsulated ingredients in the host material, prolong the shelf life of the encapsulated ingredients, expedite the absorption kinetics (e.g., onset time) after consumption, or enhance the bioavailability of the encapsulated ingredients.
41. Oral Drug Delivery Device with Biodegradable Metal Alloy Penetration Mechanism
BIOGRAIL APS, 2023
A delivery device for oral administration of low-permeability drugs, comprising a body and a delivery part with a first attachment part that penetrates the gastrointestinal wall to release the drug. The first attachment part is made of a biodegradable metal alloy, such as magnesium, iron, or zinc, and is designed to degrade in the body after drug release. The device can be contained in a pharmaceutical composition, such as a capsule or suppository, and is targeted to deliver the drug at specific sites in the gastrointestinal tract.
42. Protective Effect of Lactiplantibacillus plantarum subsp. plantarum SC-5 on Dextran Sulfate Sodium—Induced Colitis in Mice
Ruoran Shi, Fazheng Yu, Xueyu Hu - MDPI AG, 2023
Inflammatory bowel disease (IBD) is a specific immune-associated intestinal disease. At present, the conventional treatment for patients is not ideal. Probiotics are widely used in the treatment of IBD patients due to their ability to restore the function of the intestinal mucosal barrier effectively and safely. Lactiplantibacillus plantarum subsp. plantarum is a kind of probiotic that exists in the intestines of hosts and is considered to have good probiotic properties. In this study, we evaluated the therapeutic effect of Lactiplantibacillus plantarum subsp. plantarum SC-5 (SC-5) on dextran sulfate sodium (DSS)-induced colitis in C57BL/6J mice. We estimated the effect of SC-5 on the clinical symptoms of mice through a body weight change, colon length, and DAI score. The inhibitory effects of SC-5 on the levels of cytokine IL-1, IL-6, and TNF- were determined by ELISA. The protein expression levels of NF-B, MAPK signaling pathway, and the tight junction proteins occludin, claudin-3, and ZO-1 were verified using Western Blot and immunofluorescence. 16S rRNA was used to verify the ... Read More
43. Colonic Transendoscopic Enteral Tubing Is a New Pathway to Microbial Therapy, Colonic Drainage, and Host–Microbiota Interaction Research
Weihong Wang, Gaochen Lu, Xia Wu - MDPI AG, 2023
The limitation of traditional delivery methods for fecal microbiota transplantation (FMT) gave birth to colonic transendoscopic enteral tubing (TET) to address the requirement of frequent FMTs. Colonic TET as a novel endoscopic intervention has received increasing attention in practice since 2015 in China. Emerging studies from multiple centers indicate that colonic TET is a promising, safe, and practical delivery method for microbial therapy and administering medication with high patient satisfaction. Intriguingly, colonic TET has been used to rescue endoscopy-related perforations by draining colonic air and fluid through the TET tube. Recent research based on collecting ileocecal samples through a TET tube has contributed to demonstrating community dynamics in the intestine, and it is expected to be a novel delivery of proof-of-concept in hostmicrobiota interactions and pharmacological research. The present article aims to review the concept and techniques of TET and to explore microbial therapy, colonic drainage, and microbial research based on colonic TET.
44. Polymer-Coated Hard Shell Capsule with Methacrylate Copolymer and pH-Responsive Release Mechanism
EVONIK OPERATIONS GMBH, 2023
A polymer-coated hard shell capsule for targeted drug release, comprising a hard shell capsule body and cap, coated with a solution containing a methacrylate copolymer, an alkali salt of a saturated aliphatic monocarboxylic acid, glycerol monostearate, and a plasticizer. The coating composition accelerates release of the active ingredient at a pH of 7.2, enabling fast release in the colon.
45. Advances in Polysaccharide-Based Oral Colon-Targeted Delivery Systems: The Journey So Far and the Road Ahead
Ibrahim M. Ibrahim - Springer Science and Business Media LLC, 2023
Various colon-targeted oral delivery systems have been explored so far to treat colorectal diseases, including timed-release systems, prodrugs, pH-based polymer coatings, and microflora-triggered systems. Among them, the microbially triggered system has gained attention. Among various oral colon-targeted delivery systems discussed, the polysaccharide-based colon-targeted delivery system has been found to be quite promising as polysaccharides remain unaffected by gastric as well as upper intestine milieu and are only digested by colonic bacteria upon reaching the colon. The major bottleneck associated with this delivery is that non-suitability of this system during the diseased state due to decrease in bacterial count at that time. This causes the failure of delivery system to release the drug even at colonic site as the polysaccharide matrix/coat cannot be digested properly due to lack of bacteria. The co-administration of probiotics is reported to compensate for the bacterial loss besides facilitating site-specific release. However, this research is also limited at the preclinical l... Read More
46. Microbiota-sensitive drug delivery systems based on natural polysaccharides for colon targeting
Hajar Azehaf, Youcef Benzine, Madjid Tagzirt - Elsevier BV, 2023
Colon targeting is an ongoing challenge, particularly for the oral administration of biological drugs or local treatment of inflammatory bowel disease (IBD). In both cases, drugs are known to be sensitive to the harsh conditions of the upper gastrointestinal tract (GIT) and, thus, must be protected. Here, we provide an overview of recently developed colonic site-specific drug delivery systems based on microbiota sensitivity of natural polysaccharides. Polysaccharides act as a substrate for enzymes secreted by the microbiota located in the distal part of GIT. The dosage form is adapted to the pathophysiology of the patient and, thus, a combination of bacteria-sensitive and time-controlled release or pH-dependent systems can be used for delivery.
47. Microalgal biomass-assisted delivery of probiotics for modulation of gut homeostasis and alleviation of intestinal inflammation
Ziyi Han, Cheng Zhang, Jiaxin An - Elsevier BV, 2023
The clinical application of orally delivered probiotics as live therapeutics in the treatment of colitis is hampered by suboptimal bacterial bioactivity and inadequate gut retention. Here, we present a novel symbiotic approach that combines Spirulina microalgae and probiotics (SP@BC) to enhance the therapeutic efficacy of bacteriotherapy. The SP@BC is established by attaching chitosan-coated probiotic strains (BCCS) on Spirulina platensis (SP) via electrostatic self-assembly. Following oral administration, the natural antioxidative bioenzymes present in SP can persistently protect probiotics from oxidative damage in inflamed intestines. Furthermore, the helical-shaped SP can be easily trapped by the intestinal villi, resulting in a significantly enhanced gut retention of the SP@BC system. In a mouse model of colitis, orally administrated SP@BC distinctly improves intestinal permeability, reduces gut inflammation, and restores intestinal microbial homeostasis. The microalgae-assisted delivery of probiotics is highly effective, safe, and easily manufacturable, showcasing promising pote... Read More
48. Polymeric carriers in probiotic delivery system
Heenu Sharma, Swati Sharma, Jasveen Bajwa - Elsevier BV, 2023
Probiotics are good microbes that have the potential to improve the health of host when administered in proper quantity. They help to prevent and treat gastro-intestinal problems, allergies, colon cancer, diabetes, inflammation and enhance immunity. However, the applications of probiotics are limited because of their poor viability during the time of processing, storage as well as delivery in the gastro-intestine tract. So, in order to overcome these limitations of probiotics, probiotic delivery systems have received much attention. This review targeted the different types of polymers that are employed as a carrier system for probiotic delivery system because of their excellent properties including biodegradability, less toxicity and biocompatibility which helps to prolong the viability of strains of probiotic in harsh conditions of gut system of host.
49. A Review on Colon Drug Delivery Systems
Karra Geetha, Sara Akshitha, T. Rama Rao - Global Research Online, 2023
Colon-specific drug delivery systems have garnered significant attention in recent years due to their potential to overcome the limitations associated with conventional drug delivery routes.These systems aim to target drugs specifically to the colon, thereby enhancing therapeutic efficacy while minimizing systemic side effects.This review provides a comprehensive overview of the various colon drug delivery systems developed and explores their advantages, challenges, and future prospects.Additionally, recent advancements in this field, including novel approaches and emerging technologies, are discussed.The review concludes with an emphasis on the importance of further research and development in colon drug delivery systems to meet the evolving needs of pharmaceutical science.
50. The single-cell modification strategies for probiotics delivery in inflammatory bowel disease: A review
Mengzhen Han, Wenzhi Lei, Jingjing Liang - Elsevier BV, 2023
Oral probiotic therapy has become an increasingly attractive method for treating various diseases, including intestinal barrier dysfunction, inflammatory bowel disease (IBD), and colorectal cancer due to its safety and convenience. However, only a few probiotics after oral gavage can survive the acidic and bile salt conditions of the gastrointestinal tract and colonize the colon to have a nutritional effect on the host. To address these challenges, encapsulation technology has been applied to protect probiotics from harsh gastrointestinal conditions, improve gut adhesion, and reduce immunogenicity. In addition, some of the functional polysaccharides are used to endow probiotics with exogenous functions as prebiotics. In this review, we systematically introduced the advancements of emerging single-cell modification strategies for probiotics in IBD applications. Additionally, we discussed the limitations and perspectives of single-cell modification strategies for probiotics. This review contributed to the development of probiotic delivery systems with higher therapeutic efficacy agains... Read More
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