Mucoadhesive Polymers Research Articles

Functionalisation of chitosan with methacryloyl and crotonoyl groups as a strategy to enhance its mucoadhesive properties

Mucoadhesive polymers are crucial for prolonging drug retention on mucosal surfaces. This study focuses on synthesising and characterising novel derivatives by reacting chitosan with crotonic and methacrylic anhydrides. The structure of the resulting derivatives was confirmed using proton-nuclear magnetic resonance spectroscopy and Fourier-transform infrared spectroscopy. It was established that the degree of substitution plays a crucial role in the pH-dependent solubility profiles and electrophoretic mobility of the chitosan derivatives. Spray-drying chitosan solutions enabled preparation of microparticles, whose mucoadhesive properties were evaluated using fluorescence flow-through studies and tensile test, demonstrating improved retention on sheep nasal mucosa for modified derivatives. Acute toxicity studies conducted in vivo using planaria and in vitro using MTT assay with the Caco-2 cell line, a model of the mucosal epithelium in vitro, showed that the novel derivatives are not cytotoxic. These findings emphasise the potential of tailored chitosan chemical modifications for enhancing transmucosal drug delivery.

Technological Strategies Applied to Pharmaceutical Systems for Intranasal Administration of Drugs Intended for Neurological Treatments: A Review.

The complexity of treating neurological diseases has meant that new strategies have had to be developed to deliver drugs to the brain more efficiently and safely. Intranasal drug delivery is characterized by its ease of administration, safety, and rapid delivery directly from the nose to the brain. Several strategies have been developed to improve the delivery of drugs to the brain via nasal administration. These include the use of mucoadhesive and thermoresponsive polymers and their combination into polymer blends, as well as the use of liposomes, niosomes, and nano- and microemulsions. Therefore, this review focuses on technologies for developing pharmaceutical systems aimed at delivery via the nose to the brain, contributing to new treatments for difficult neurological disorders. Some of the most common and difficult-to-treat neurological conditions, the intranasal route of administration, and the anatomy of the nasal cavity have been discussed, as well as factors that may influence the absorption of drugs administered into the nose. The types of intranasal formulations and the devices that can be used to administer these products are also discussed in this review. Strategies for improving the transport of bioactive agents and increasing bioavailability are highlighted. The technologies discussed in this review can facilitate the development of formulations with improved properties, such as drug release and mucoadhesiveness, which have several advantages for patients requiring complex neurological treatments.

The effect of mucoadhesive polymers on ocular permeation of thermoresponsive in situ gel containing dexamethasone–cyclodextrin complex

Dexamethasone (DXM) is a commonly used corticosteroid in the treatment of ocular inflammatory conditions that affect more and more people. The aim of this study was to evaluate the effect of the combination of hydroxypropyl-β-cyclodextrin (HPBCD), in situ gelling formulations, and other mucoadhesive polymers, i.e., hydroxypropyl methylcellulose (HPMC) and zinc-hyaluronate (ZnHA), on permeation by applying in vitro and ex vivo ophthalmic permeation models. Additionally, gelling properties, in vitro drug release, and mucoadhesion were measured to determine the impact of these factors on permeation and ultimately on bioavailability. The results showed that GEL1 and GEL2 had an optimal gelling temperature, 36.3 ℃ and 34.6 ℃, respectively. Moreover, the combination of Poloxamer 407 (P407) with other polymers improved the mucoadhesion (GEL1: 1333.7 mN) compared with formulations containing only P407 (P12: 721.8 mN). Both HPBCD and the gel matrix had a considerable influence on the drug release and permeability of DXM, and the combination could facilitate the permeation into the aqueous humor. After 30 min of treatment, the DXM concentration in the aqueous humor was 1.16–1.37 µg∕mL in case of the gels, whereas DXM could not be detected when treated with the DXM suspension. The results of the experiments using an in vitro cell line indicated that the formulations could be considered safe for topical treatment of the eye. In conclusion, with application of a small amount of HPMC (0.2 % w∕w), the concentration of P407 could be reduced to 12 % w/w while maintaining the ideal gelling properties and gel structure without negatively affecting permeability compared with the formulation containing a higher amount of P407. Furthermore, the gel matrix may also provide programmed and elongated drug release.

Zein and 3-Aminophenyl Boronic Acid Conjugated Polyvinylpyrrolidone Polymer Blend: Electrospinning, Characterization, and Mucoadhesive Drug Delivery.

The era of mucoadhesive polymers has advanced to the next generation, focusing on targeted adhesion of chemical functional groups with mucosa. This work aims to develop boronic acid functionalized polymers, which could facilitate reversible binding with the mucin in the mucosa. Pendant groups of boronic acid were conjugated on the chains of polyvinylpyrrolidone (PVP) via C═N bonding. The evidence from FTIR spectroscopy, XPS analysis, and UV spectroscopy has been used for the confirmation of the chemical conjugation of 3-aminophenyl boronic acid (APBA) to PVP. Boronate ester formation is a pH-dependent process. High pKa values of APBA preferably cause the binding of trigonal-shaped boronic acid with sialic acid groups of mucin. Boronic acid moieties additionally benefited in mucoadhesion in comparison to PVP alone, which is a result of the formation of a five-membered boronate ester complex. The presence of boronic acid moieties enhanced the force of adhesion on porcine buccal mucosal tissue from 13.12 ± 1.52 to 19.04 ± 1.97 g force. Specific binding of the polymer to the mucosal surface caused prolonged adhesion of the polymer to the mucosal surface. A polymer blend of boronic acid functionalized PVP and zein has been explored for its potential for mucoadhesive delivery of propranolol hydrochloride.

To Explore Nasal-Brain Lymphatic System for Brain-Targeted Drug Delivery and to Treat Neurodegenerative Diseases.

Brain-related Neurodegenerative Disorders (NDD) are the leading cause of low life expectancy globally. Brain-targeted drug delivery is required for treating most the NDD via bypassing the blood-brain barrier, and hepatic first-pass metabolism. The nasal-brain drug delivery route has the advantage of locally enhancing drug delivery to the brain, mainly through the olfactory route rather than systemic circulation. To overcome the limitations of nasal-brain drug delivery, a nanocarrier approach and mucoadhesive polymers are needed. Notwithstanding these constraints, various nanotechnology techniques have been created, including polymeric micelles, liposomes, polymeric nanoparticles, solid lipid nanoparticles, & nano-emulsions. This review aims to explore the intranasal pathway for drug delivery through the nasal-brain lymphatic systems, considering brain anatomy and physiology along with a drug formulation design approach.

Development of synergistic antifungal in situ gel of miconazole nitrate loaded microemulsion as a novel approach to treat vaginal candidiasis

Limited solubility is the main cause of the low local availability of anti-candidiasis drug, miconazole nitrate (MN). The study’s objective was to develop and characterize microemulsion (ME) based temperature-triggered in situ gel of MN for intravaginal administration to enhance local availability and antifungal activity. The solubility of MN was initially studied in different oils, surfactants, and co-surfactants. Then, pseudo-ternary phase diagrams were constructed to select the best ratio of various components. The ME formulations were characterized by thermodynamic study, droplet size, polydispersity index (PDI), viscosity, and in-vitro antifungal mean inhibition zone (MIZ). Selected MEs were incorporated into different in situ gel bases using a combination of two thermosensitive polymers (poloxamer (PLX) 407 and 188), with 0.6% of hydroxypropyl methylcellulose (HPMC K4M) and gellan gum (GG) as mucoadhesive polymer. ME-based gels (MG) were investigated for gelation temperature, gelation time, viscosity, spreadability, mucoadhesive strength, in vitro release profile, and MIZ test. Furthermore, the optimum MG was assessed for in vivo animal irritation test and FESEM investigation. Tea tree oil, lavender oil, tween 80, and propylene glycol (PG) were chosen for ME preparation for the optimal formulation; formulation ME7 and ME10 were chosen. After incorporation of the selected formulation into a mixture of P407 and P188 (18:2% w/w) with 0.6% mucoadhesive polymer, the resultant MG formulation (MG1) revealed optimum gelation temperature (33 ± 0.01℃) and appropriate viscosity with enhanced sustained release (98%) and retention through sheep vaginal mucosa, MG1 exhibited a better MIZ compared to the 2% MN gel formulation and the marketed MN product, and no rabbit vagina irritation. In conclusion, the miconazole nitrate-loaded MG-based formula sustained the duration of action and better antifungal activity than the marketed miconazole nitrate formulation.

Poly(Lactic-co-Glycolic Acid Nanoparticles Loaded with Docetaxel and Coated with Chitosan, Carboxymethyl Chitosan, or Glycol Chitosan.

Docetaxel (DTX) is a chemotherapeutic drug that has high toxicity and low bioavailability. To solve these problems, PLGA nanoparticles (NPs) were loaded with DTX and coated with mucoadhesive polymers; chitosan (CS), carboxymethyl chitosan (CMCS), or glycol chitosan(GCS). The NPs were characterized for size, charge, and polydispersity. The particles were explored using SEM, FTIR, DSC, and XRD. In vitro studies were performed to evaluate the mucoadhesive properties of the NPs and the drug release. The results validated the successful formation of spherical and monodispersed DTX NPs. The coated NPs exhibited highly positive charges, reaching +44.30±0.21 mV, whereas the uncoated NPs were almost neutral. The formulations demonstrated excellent encapsulation efficiency (>98%) and loading capacity (>45%). All polymers used in the coating process enhanced the mucoadhesive properties of PLGA NPs and sustained DTX release. Both the mucoadhesiveness and release were related to the used coating polymer and its concentration. The formulations were stable for up to three months in the refrigerator. In conclusion, loading DTX in PLGA NPs and coating them with CS, CMCS, or GCS provides a promising strategy to increase the NPs' residence time on mucosal surfaces, which is expected to decrease the required dose of DTX and reduce its side effects.

Mucoadhesive poly(ethylene glycol)-based biodegradable polyesters with in-chain model drug

Mucoadhesive polymers have received significant interest in drug delivery due to the prolonged residence time on various mucus gel layers. Not only local effects but also the systemic uptake of active pharmaceutical ingredients can be enhanced by such mucoadhesive excipients. In this study, we design novel poly(ethylene glycol) based mucoadhesive polyesters bearing unsaturated or sulfhydryl functionalities and model drug fluorescein polymerized in the polymeric backbone. The structure of polyesters was confirmed via 1H NMR and FTIR, while their molar masses, determined by gel permeation chromatography, were found to be between 3.6 and 4.0 kDa. Enzymatic degradation studies showed the ability of lipase to degrade the polymeric chains. Because of the mucoadhesive groups, the viscosity of mucus mixtures with these polymers increased 1.8-fold for the double bond, while 4.3-fold for thiol functional polymers, compared to PEG. Prolonged residence time on porcine intestinal mucosa was detected, as 3 h after application, up to 69 % of the polymers were still on the mucosa, whereas PEG was completely removed within 30 mins. Highly pH and enzyme-dependent release of fluorescein was noticed; only pH > 6.8 caused significant drug release. According to the results of this study, PEG-based unsaturated and thiolated polyesters with in-chain model drugs are great mucoadhesive and biodegradable drug carriers with sustained release properties.

Design of an oral formulation combining PVA nanofibers and PEGylated liposomes for enhanced drug delivery

Modifying the surface properties of nanoparticles is crucial for enhancing the oral absorption of encapsulated drugs. Although both mucoadhesion and mucus permeability are essential properties for improving oral absorption, their opposing characteristics render their combination in a single formulation challenging. The present study aimed to integrate both strategies and design a novel oral formulation by creating nanofibers from a mucoadhesive polymer solution containing approximately 100 nm PEGylated liposomes. First, we evaluated the physicochemical properties of PEGylated liposomes released from nanofibers made of sodium carboxymethylcellulose (CMC-Na) and polyvinyl alcohol (PVA), as well as from PVA alone nanofibers. Liposomes released from CMC-Na/PVA nanofibers had a particle size of 533.9 ± 85.0 nm, showing aggregation, while those from PVA nanofibers maintained a particle size without aggregation (142.8 ± 7.31 nm). To increase the liposome content in PVA nanofibers, we used hydroxypropyl-β-cyclodextrin (HPβCD) as a cryoprotectant, converting the suspension to powder and increasing liposome content by approximately 30-fold. PVA nanofibers increasing liposome content had a fiber diameter of 355.5 ± 77.1 nm, and liposomes released from nanofibers retained their morphology. We then used the flow-through method to evaluate the formulation's adhesive properties, and our findings confirmed its better mucosal adhesion and reduced excretion by mucus clearance (about 1/10) compared to a liposome suspension. Subsequent application to rat intestinal tissue showed that the mucus partially dissolved the nanofibers, allowing PEGylated liposomes to penetrate the mucus layer. Oral administration to rats showed improved gastrointestinal retention, thereby confirming that this novel oral formulation may improve drug oral absorption.

Advances in Chitosan-Based Smart Hydrogels for Colorectal Cancer Treatment

Despite advancements in early detection and treatment in developed countries, colorectal cancer (CRC) remains the third most common malignancy and the second-leading cause of cancer-related deaths worldwide. Conventional chemotherapy, a key option for CRC treatment, has several drawbacks, including poor selectivity and the development of multiple drug resistance, which often lead to severe side effects. In recent years, the use of polysaccharides as drug delivery systems (DDSs) to enhance drug efficacy has gained significant attention. Among these polysaccharides, chitosan (CS), a linear, mucoadhesive polymer, has shown promise in cancer treatment. This review summarizes current research on the potential applications of CS-based hydrogels as DDSs for CRC treatment, with a particular focus on smart hydrogels. These smart CS-based hydrogel systems are categorized into two main types: stimuli-responsive injectable hydrogels that undergo sol-gel transitions in situ, and single-, dual-, and multi-stimuli-responsive CS-based hydrogels capable of releasing drugs in response to various triggers. The review also discusses the structural characteristics of CS, the methods for preparing CS-based hydrogels, and recent scientific advances in smart CS-based hydrogels for CRC treatment.

Design, Optimization and Performance Assessment of Memantine Buccal Films for Targeted Drug Delivery.

Memantine is primarily prescribed for treating moderate to severe Alzheimer’s disease by modulating glutamate, a key neurotransmitter involved in cognitive functions like memory and learning. By blocking excessive glutamate activity at NMDA receptors, memantine helps improve cognitive function and slow symptom progression in Alzheimer’s patients. In this study, solvent evaporation was used in the formulation of memantine in order to increase its bioavailability and sustain its release. Chitosan, HPMC, a mucoadhesive polymer, carbopol, a sensitive to pH polymer and propyle glycol, a permeation enhancer, were all incorporated in the formulation. All formulations underwent evaluation for moisture content, folding endurance, swelling index, mucoadhesive strength and drug content. Drug release profiles were assessed through in-vitro diffusion studies. Results indicated that increasing concentrations of polymers led to higher mucoadhesive strength, consequently enhancing Memantine release from the system. The optimal formulation(F9), with carefully balanced polymer concentrations, demonstrated more resident time, sustained drug release and improved bioavailability.

Development and Evaluation of Oromucosal Spray Formulation Containing Plant-Derived Compounds for the Treatment of Infectious and Inflammatory Diseases of the Oral Cavity.

According to data in the literature, natural products and essential oils are often used in dental practice. To develop a new oromucosal spray for the treatment of infectious and inflammatory diseases of the oral cavity, clove CO2 extract and essential oils of lavender and grapefruit were used as active pharmaceutical ingredients. Clove extract was obtained by the method of subcritical extraction from various raw materials, the choice of which was based on the yield of the CO2 extract and the study of its phytochemical and microbiological properties. Based on the results of microscopic and diffraction analyses, the rational time of ultrasonic exposure for the emulsion of active pharmaceutical ingredients was established. Mucoadhesive polymers were used as stabilizers of the two-phase system and prolongators. This article discusses the impact of the type and concentration of mucoadhesive polymers on the stability of the emulsion system; the viscous, textural, adhesive, and film characteristics of oromucosal spray; and the parameters determining sprayability.

Formulation Variables Influencing the Development of Ketoconazole Gastroretentive Drug Delivery System

Background: Ketoconazole (KZ) is categorized as class II according to the Biopharmaceutics Classification System (BSC) classification, which shows a strong pH-dependent solubility where its solubility is enhanced under an acidic medium (pH below 3). This strong pH dependence results in unpredictable absorption and a wide range of bioavailabilities. Objective: To prolong the gastric residence time of KZ’s tablet to enhance KZ’s solubility and hence its bioavailability for better therapeutic activity. Methods: To prepare mucoadhesive tablets, we use both direct and wet granulation methods. We employed various evaluation tests to assess the prepared tablets. These tests encompass a range of assessments, including weight variation, hardness, thickness, friability, disintegration test, swelling study, mucoadhesive strength study, and in vitro drug release studies. Results: The study found that polymer viscosity, as well as polymer concentration, have a significant effect on mucoadhesive strength and drug release, whereas diluent type has a non-significant influence on drug release. We selected Formula 7, which employs xanthan gum as a mucoadhesive polymer in a 1:1 drug polymer ratio, as the optimum formula because it provides an accepted physico-mechanical property and releases 87% of the drug over 8 hours. Conclusions: Gastric mucoadhesive tablets may be an effective method of delivering active ingredients, as they provide a favorable environment that enhances their dissolution by extending their duration in the stomach, thereby increasing their bioavailability.

Formulation and evaluation of bioadhesive buccal Films of Domperidone co-crystals by using Tamarind kernel powder as mucoadhesive polymer

As solubility plays key role in drug dissolution and bioavailability lots of techniques to enhance solubility are evolved. One of the techniques is co crystallization. The main aim of the work is to enhance the solubility of domperidone by co crystallization using coformers like Para amino benzoic acid and succinic acid. The cocrystals were evaluated for melting point and solubility enhancement. these cocrystals were used to prepare buccal films by solvent casting method. In the preparation of buccal films Tamarind kernel powder obtained from the seeds of Tamarind is used as mucoadhesive polymer and Hydroxy propyl methyl cellulose as film former, Polyethylene glycol 6000 as plasticizer, dehydrated banana powder as super disintegrant, sodium saccharin as sweetener and mixture of ethanol and water as solvents. The mucoadhesive strength of Tamarind kernel powder was determined using modified physical balance method. Four buccal films were prepared in which PDBF1 and PDBF2 are the two buccal films prepared using cocrystals of domperidone and Para amino benzoic acid and other two buccal films SDBF1 and SDBF2 with cocrystals of domperidone and Succinic acid. The buccal films were evaluated for different tests like folding endurance, swelling index and Surface pH. In vitro diffusion studies were conducted by Franz diffusion cell using egg membrane as semipermeable membrane and phosphate buffer of pH 7.4. The buccal films prepared with cocrystals of domperidone and succinic acid at weight ratio 1:2 has shown 86%drug release. The work has concluded that there is fold increase in aqueous solubility of Domperidone and the optimized formula is SDBF2 and Tamarind kernel powder can be used as mucoadhesive polymer in novel drug delivery systems. Keywords: co crystals, solvent evaporation, muco adhesive, buccal films, solvent evaporation

Formulation and Evaluation of Colon Targeted Mucoadhesive Microsphere of Aceclofenac

The aim of this research was to formulate and evaluate colon-targeted mucoadhesive microspheres of aceclofenac, an anti-inflammatory drug, to enhance its bioavailability and reduce gastrointestinal side effects. Aceclofenac- loaded microspheres were prepared using a variety of mucoadhesive polymers such as chitosan, sodium alginate, and Eudragit. The prepared microspheres were characterized for particle size, surface morphology, drug encapsulation efficiency, in vitro drug release, and mucoadhesion properties. The optimized formulation demonstrated a sustained drug release profile, efficient mucoadhesion, and enhanced stability in simulated colonic fluid. The findings suggest that mucoadhesive microspheres are a promising carrier for the targeted delivery of aceclofenac to the colon.

A REVIEW ON BASIC PRINCIPLES OF MUCOADHESION: THE IMPORTANCE OF CHITOSAN AS A MUCOADHESIVE BIOPOLYMER

Mucoadhesive polymers have the special functions which lead to adhesion to the mucin/ epithelial surface on the mucus-covered areas in the body such as eye, nose, vaginal and buccal cavities, and GI tract. Therefore, they provide to increase the residence time of the dosage form on the mucosa and to significantly improve the drug administration. Mucoadhesive drug delivery systems containing chitosan and its modified derivatives have many advantages for both local and systemic drug delivery. The goal of this review is to put forward the importance of chitosan as a functionalized mucoadhesive drug delivery system.

Intranasally Inoculated SARS-CoV-2 Spike Protein Combined with Mucoadhesive Polymer Induces Broad and Long-Lasting Immunity.

Current mRNA vaccines against SARS-CoV-2 effectively induce systemic and cell-mediated immunity and prevent severe disease. However, they do not induce mucosal immunity that targets the primary route of respiratory infection, and their protective effects wane after a few months. Intranasal vaccines have some advantages, including their non-invasiveness and the additional ability to activate mucosal immunity. In this study, we aimed to explore the effectiveness of an intranasally inoculated spike protein of SARS-CoV-2 mixed with a carboxy-vinyl polymer (S-CVP), a viscous agent. Intranasally inoculated S-CVP strongly induced antigen-specific IgG, including neutralizing antibodies, in the mucosal epithelium and serum and cellular immunity compared to the spike protein mixed with aluminum potassium sulfate. Furthermore, IgA production was detected only with S-CVP vaccination. S-CVP-inoculation in mice significantly suppressed the viral load and inflammation in the lung and protected mice against SARS-CoV-2 challenges, including an early circulating strain and the Omicron BA.1 variant in a manner dependent on CD8+ cells and monocytes/neutrophils. Surprisingly, high antibody responses and protective effects against multiple variants of SARS-CoV-2, including Omicron BA.5, persisted for at least 15 months after the S-CVP immunization. Hence, we propose intranasal inoculation with S-CVP as a promising vaccine strategy against SARS-CoV-2.

Formulation, Optimization and In-Vivo Characterization of Thermosensitive In-Situ Nasal Gel Loaded with Bacoside a for Treatment of Epilepsy.

The intranasal route has demonstrated superior systemic bioavailability due to its extensive surface area, the porous nature of the endothelial membrane, substantial blood flow, and circumvention of first-pass metabolism. In traditional medicinal practices, Bacopa monnieri, also known as Brahmi, is known for its benefits in enhancing cognitive functions and potential effects in epilepsy. This study aimed to develop and optimize a thermosensitive in-situ nasal gel for delivering Bacoside A, the principal active compound extracted from Bacopa monnieri. The formulation incorporated Poloxamer 407 as a thermogelling agent and HPMC K4M as the Mucoadhesive polymer. A 32-factorial design approach was employed for Optimization. Among the formulations. F7 exhibited the most efficient Ex-vivo permeation through the nasal mucosa, achieving 94.69 ± 2.54% permeation, and underwent a sol-gel transition at approximately 30.48°C. The study's factorial design revealed that gelling temperature and mucoadhesive strength were critical factors influencing performance. The potential of in-situ nasal Gel (Optimized Batch-F7) for the treatment of epilepsy was demonstrated in an in-vivo investigation using a PTZ-induced convulsion model. This formulation decreased both the occurrence and intensity of seizures. The optimized formulation F7 showcases significant promise as an effective nasal delivery system for Bacoside A, offering enhanced bioavailability and potentially increased efficacy in epilepsy treatment.

Hard Gelatin Capsules with Alginate-Hypromellose Microparticles as a Multicompartment Drug Delivery System for Sustained Posaconazole Release.

Microparticles as a multicompartment drug delivery system are beneficial for poorly soluble drugs. Mucoadhesive polymers applied in microparticle technology prolong the contact of the drug with the mucosa surface enhancing drug bioavailability and extending drug activity. Sodium alginate (ALG) and hydroxypropyl methylcellulose (hypromellose, HPMC) are polymers of a natural or semi-synthetic origin, respectively. They are characterized by mucoadhesive properties and are applied in microparticle technology. Spray drying is a technology employed in microparticle preparation, consisting of the atomization of liquid in a stream of gas. In this study, the pharmaceutical properties of spray-dried ALG/HPMC microparticles with posaconazole were compared with the properties of physical mixtures of powders with equal qualitative and quantitative compositions. Posaconazole (POS) as a relatively novel antifungal was utilized as a model poorly water-soluble drug, and hard gelatin capsules were applied as a reservoir for designed formulations. A release study in 0.1 M HCl showed significantly prolonged POS release from microparticles compared to a mixture of powders. Such a relationship was not followed in simulated vaginal fluid (SVF). Microparticles were also characterized by stronger mucoadhesive properties, an increased swelling ratio, and prolonged residence time compared to physical mixtures of powders. The obtained results indicated that the pharmaceutical properties of hard gelatin capsules filled with microparticles were significantly different from hard gelatin capsules with mixtures of powders.

Stability of Free and Liposomal Encapsulated RNA on a Mucoadhesive PVA Polymer for Esophageal RNA Drug Targeting Using the EsoCap System

AbstractThe development of RNA and oligonucleotide‐based therapeutics is a longstanding goal and is currently gaining significant attention. Several RNA‐based drugs are approved for clinical use. Others are under investigation or in preclinical trials. This study have initiated the development of RNA drugs for localized use in the esophagus, utilizing the EsoCap System. This system's core component is a mucoadhesive film that carries the RNA drug and is precisely applied to the esophagus. Research into the stability and properties of naked and liposomal‐encapsulated RNA on mucoadhesive polymer film reveals that RNAs remain stable in various conditions without degradation, RNA leakage, or liposome fusion observed. The liposome size also remains constant after application on the film, drying, and rehydration. These findings pave the way for RNA drug development for esophageal diseases and their administration via the EsoCap system.