Fig 1 - uploaded by Vitaliy V Khutoryanskiy
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Oral mucosa and lingual papillae. Keratinised masticatory mucosa covers the gingiva, hard palate, and dorsum of the tongue. The non-keratinised lining mucosa covers the rest of the mouth surface including: the lips, cheeks, and soft palate. Regions of taste buds in the lingual papillae are covered by a specialised mucosa, containing nerve endings enabling sensory perception. There are four types of lingual papillae: circumvallate papillae are large dome-shaped papillae towards the rear of the tongue, which are surrounded by a serous secretion produced by adjacent Von Ebner's glands; foliate papillae are folds on the sides of the rear of the tongue, contain taste buds, and are covered by non-keratinised mucosa; fungiform papillae are found mostly on the front of the tongue, are covered by non-keratinised mucosa, and contain taste buds; filiform papillae are very small, keratinised, and are the most numerous papillae type, covering most of the dorsal surface, however they do not contain taste buds.
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The role of mucoadhesion in the perception and sensory characterisation of food products is becoming more apparent. Traditionally, mucoadhesives are used to enhance drug permeability and retention at mucosal membranes in the body, by adherence to a mucosal membrane formed through various interactions between the mucoadhesive and proteins present in...
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... The human gastric epithelial cell line NCI-N87, comprising mucus-secreting cells that are histologically relevant to the site of action of the product, was used to evaluate the bioadhesive properties of Poliprotect (F) . Numerous methods have been proposed and are used to evaluate the mucoadhesive properties of different formulations [63][64][65][66]. The inclined plane method is based on previous work reported in specific references in the literature, and it measures mucoadhesiveness as a function of the retention of the mucoadhesive formulation in contact with a substrate. ...
When the protective mechanisms of the gastroesophageal mucosa are overwhelmed by injurious factors, the structural and functional mucosal integrity is compromised, resulting in a wide spectrum of disorders. Poliprotect has recently been shown to be non-inferior to standard-dose omeprazole for the treatment of endoscopy-negative patients with heartburn and/or epigastric pain or burning. Here, we provide preclinical data describing the mechanism of action of the Poliprotect formulation, a 100% natural, biodegradable, and environmental friendly medical device according to EU 2017/745 and containing UVCB (unknown or variable composition, complex-reaction products, or biological materials) substances of botanical and mineral origin, according to the REACH and European Chemical Agency definitions. Different in vitro assays demonstrated the capability of Poliprotect to adhere to mucus-secreting gastric cells and concomitantly deliver a local barrier with buffering and antioxidant activity. In studies conducted in accordance with systems biology principles, we evaluated the effects of this barrier on human gastric cells exposed to acidic stress. Biological functions identified via Ingenuity Pathway Analysis highlighted the product’s ability to create a microenvironment that supports the mucosal structural and functional integrity, promotes healing, and restores a balanced mucosal inflammatory status. Additionally, transepithelial electrical resistance and an Ussing chamber showed the product’s capability of preserving the integrity of the gastric and esophageal epithelial barriers when exposed to an acid solution. Two in vivo models of erosive gastropathy further highlighted its topical protection against ethanol- and drug-induced mucosal injury. Overall, our findings sustain the feasibility of a paradigm shift in therapeutics R&D by depicting a very innovative and desirable mode of interaction with the human body based on the emerging biophysical, rather than the pharmacological properties of these therapeutic agents.
... The current literature categorizes methods for evaluating mucoadhesion into direct and indirect approaches [28]. Direct methods involve measuring the force or time required to detach a formulation from a mucosal membrane or a mucosa-mimicking substrate. ...
The study focuses on the development of an in situ gelling dexamethasone (DEX) oromucosal formulation designed for the treatment of aphthous stomatitis. Three series of formulations were prepared; a first series containing DEX suspended, a second series containing DEX and, in addition, mint essential oil (EO), and a third series containing EO and DEX solubilized in propylene glycol (PG). In the composition, polymers in the role of mucoadhesive agent were interchanged (hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), hydroxyethyl cellulose (HEC), methyl cellulose (MC), carboxymethyl cellulose (CMC), and sodium carboxymethyl cellulose (NaCMC). Specifically, DEX was incorporated at a concentration of 0.1% (w/w) in each formulation. The influence of mint EO and DEX solubilization on the physical properties (pH measurements, rheological analysis, swelling ability, and texture analysis) and in vitro drug release was studied. Key findings revealed that HPMC-based formulation containing mint EO and PG exhibited best swelling properties (700 ± 46% after 5 h), adequate adhesiveness and in vitro drug release (34.7 ± 5.9%). Furthermore, the irritation potential assessed via the hen’s egg test on the chorioallantoic membrane (HET-CAM) demonstrated low irritancy risk. Finally, Fourier-transform infrared spectroscopy (FT-IR) showed no incompatibility between DEX and excipients. Overall, the research highlights the potential of mucoadhesive systems in improving the therapeutic efficacy of oromucosal drug delivery for managing painful oral lesions.
... Intestinal epithelial intercellular channels are restricted by a combination of tightly linked protein complexes, cellular bridges, and adherens junctions, whereas chitosan transiently opens tight junctions to increase penetration of the drug into the paracellular pathway, and this process is reversible [172]. Sodium alginate is a PH-sensitive anionic polysaccharide and is adhesive, interacting with the mucus layer through hydrogen bonding and van der Waals forces [173]. Yang and colleagues prepared chitosan sodium alginate gel nanoparticles loaded with exenatide using sodium tripolyphosphate as a cross-linking agent. ...
Diabetes is a global disease that can lead to a range of complications. Currently, the treatment of type 2 diabetes focuses on oral hypoglycemic drugs and insulin analogues. Studies have shown that drugs such as oral metformin are useful in the treatment of diabetes but can limit the liver’s ability to release sugar. The development of glucose-lowering peptides has provided new options for the treatment of type 2 diabetes. Peptide drugs have low oral utilization due to their easy degradation, short half-life, and difficulty passing through the intestinal mucosa. Therefore, improving the oral utilization of peptide drugs remains an urgent problem. This paper reviews the research progress of peptide drugs in the treatment of diabetes mellitus and proposes that different types of nano-formulation carriers, such as liposomes, self-emulsifying drug delivery systems, and polymer particles, should be combined with peptide drugs for oral administration to improve their absorption in the gastrointestinal tract.
... 1. Oral drug delivery system 2. Nasal drug delivery system 3. Ophthalmic drug delivery system 4. Vaginal drug delivery system 5. Buccal and sublingual drug delivery system. 9 The oral mucosa has many properties which make it an attractive site for drug delivery but also provides several challenges for researchers investigating novel delivery techniques to overcome many different formulations including sprays, tablets, mouthwashes, gels, pastes and patches are presently used for delivery into and/or across the oral mucosa. 10 The use of various mucoadhesive polymers, such as chitosan and lectins, are utilized to increase the efficacy of drug delivery systems on mucus membranes. ...
The goal of mucoadhesive drug delivery systems (MDDS) is to improve drug delivery effectiveness by adhering to the body's mucosal tissues. The material used in this approach adheres to mucosal surfaces, including those in the mouth, gastrointestinal system, nasal passages, and vaginal walls. The most important goal is to extend the medication's residence duration at the absorption site in order to improve drug absorption and provide a more regulated and prolonged release. Mucoadhesion refers to the adhesion between two materials, one of which is biological, through interfacial forces over an extended period. This characteristic provides an effective solution to challenges in traditional drug delivery systems, such as avoiding first-pass metabolism and facilitating localized delivery of biomolecules, including proteins, peptides, and oligonucleotides. It holds significant promise for delivering compounds via routes like ocular, nasal, vaginal, and buccal administration This study addresses the introduction, benefits, drawbacks, mechanisms, and theories of mucoadhesion in addition to polymer categorization, mucoadhesive dosage forms, assessment, and factors affecting mucoadhesion and several kinds of mucoadhesive dosage forms. Keywords: Mucoadhesion, Theories, Mucoadhesive Dosage Form, bio adhesion
... The displacement distance was measured in centimeters for up to 2 h, with the adhesion potential being inversely proportional to the sample's displacement. On the other hand, for the flow-through method (Chen et al., 2018;Cook et al., 2017;Khutoryanskiy, 2011;Syed et al., 2022), a modified apparatus was utilized. All petri dishes were inclined at a 60 • angle, and the flow of the SNES was maintained through a peristaltic pump with a flow rate of 2 mm/min (Illum, 2006;Inoue et al., 2018) to wash off the formulation from the surface of agar-mucin gel. ...
... The same IEP values for a silicon substrate are a consequence of the dissociation of surface silanol groups with pK = 2.5 [49][50][51]. At the same time, a significant contribution of acid-base interactions due to the formation of van der Waals and hydrogen bonds between mucin and polymers was noted in some papers [52,53]. ...
This study investigated the use of cellulose nanocrystals (CNC)/chitosan (Chit) polyelectrolyte complex as a stabilizing agent for Pickering emulsions. We demonstrated that chitosan reduces the surface charge of CNC improving the emulsification process. An optimal stabilizing complex containing 1% chitosan results in emulsions with minimal zeta potential (3.2 ± 0.3 mV), droplet size (2.8 ± 0.8 μm), and creaming index (19.8 ± 1.0%) values, along with high stability during storage, a change in pH, and high centrifugal forces (up to 2000 g). The study also showed that the maximum neutralized surface charge of the CNC in the CNC-Chit complex allows for effective adsorption on the surface of sunflower oil droplets, producing a denser stabilizing layer with a smaller droplet size. Additionally, chitosan addition is linked to improved stability and higher viscosity, with little dependence on ionic strength and temperature. Potentiometric titration revealed that compared with sulfated CNCs, five times less chitosan is needed to neutralize the negative surface charge of acetylated CNC. The wettability of a hydrophilic surface depends on the surface charge of the complex, and the wettability and adhesion performance increase with increasing chitosan content. Additionally, we showed that tuning the stabilizer composition can change the bioaccessibility of lipophilic compounds during oral administration.
Graphical Abstract
... (17) among the natural mucoadhesive polymers are chitosan, pectin, gelatine, sodium alginate, guar gum, and xanthan gum. (18); among the synthetic mucoadhesive polymers are cellulose derivatives, poly(acrylic acid) polymers, poly(ethylene glycol), poly(ethylene oxide), poly(vinyl pyrrolidone), and poly(vinyl alcohol). (19) numerous materials have been tested for oral biologic delivery, with varying degrees of success. ...
The majority of patients find that the oral route of drug administration is the most convenient, easy to follow, non- invasive, and physician-preferred method. However, oral biologic administration is not as beneficial as other routes because of mucosal permeability and various gastrointestinal barriers that limit the systemic absorption of complex macromolecules after ingestion. Because of their large molecular size, which results in extremely poor permeability across the intestinal mucosa, biologics are sensitive to the harsh environment of the gastrointestinal tract and thus play a significant role in the treatment of therapeutic interventions such as Chronic ailments, metabolic disease aging, and inflammatory disorders. Many drug delivery systems and pharmaceutical technologies, such as micelles, nano carriers, lipid-based carriers, and cyclodextrins, have been explored to enhance oral drug absorption. This article will first address the drug discovery, intensive research, and design that have enhanced the growth of biologics in recent decades and further accelerated the way we administer the medication in a clinical setting. physiological barriers to oral delivery of biologics and addresses various approaches to enhance the efficacy of oral delivery; furthermore, this conversation will encompass the diverse benefits and constraints of drug delivery systems as well as the general perception and promise of this emerging clinical area. Keywords: Absorption enhancers; biologics; drug delivery; Gastrointestinal barriers; insulin; microneedle pill; oral delivery.
... It is noteworthy that mucoadhesive materials are employed to dominate the fragile retention time of gels. Indisputable adhesive polymers including Carbopol, hyaluronic acid, xanthan gum, poloxamer, leads to a transition from a liquid to semisolid [7][8][9][10][11][12][13]. This feature enhances the viscosity, which results to a viable and prolonged delivery of drugs from dosage form. ...
... It lies mainly in electrostatic interaction between the positive charge of guar and negative charge present in the mucus [41]. Studies have found guar to range from being a relatively poor mucoadhesive to exhibiting good mucoadhesion [42]. This discrepancy in the claim can be explained by the species diversity of guar with different physical properties depending on the molecular weight, but also by differences in the choice of other mucoadhesive polymers compared. ...
... Acacia-containing tablets showed the lowest mucoadhesion. This result is consistent with the results of a study showing poor acacia mucoadhesion [42], despite the fact that it was not tablets but patches that were tested. Acacia is more likely to be used as a binder in the tablet formulation. ...
(1) Background: The study aimed to compare the impact of various natural polymers–sodium alginate, acacia gum, carrageenan, guar gum, xanthan gum, and tragacanth on the formulation and the physical properties of mucoadhesive vaginal tablets containing metronidazole (167 mg/g). (2) Methods: The quality of the tablets prepared by direct compression was evaluated by pharmacopoeia tests (uniformity of mass, resistance to crushing, friability). Mucoadhesion of the tablets was characterized by swelling capacity and mucoadhesive strength, i.e., the force required to detach the tablet from the rabbit mucosa. In vitro drug release was performed by a modified dissolution method in paddle apparatus containing the simulated vaginal fluid (pH 4.5). Scanning electron microscopy observed morphological changes on the swollen tablets’ surface. (3) Results: Pharmacopoeia tests have shown that all prepared tablets met the requirements on quality. The highest mucoadhesive strength was noted in tablets containing guar and xanthan gum. The highest swelling capacity was possessed by tablets containing carrageenan. (4) Conclusions: Summarizing all tests’ results, sodium alginate can be considered the most suitable natural polymer in tablet formulation. The combination of polymers providing higher mucoadhesiveness and at the same time a prolonged release, e.g., xanthan or guar, together with sodium alginate, could also be of interest.
... The mucin and cellular surfaces are often dominated by sulphated proteoglycans that provide a negative charge [33]. Further, charged nano drug conjugates more effectively bind to mucus via electrostatic interactions than neutral molecules [34]. It is hence necessary for the nano drug conjugate to be positively charged or less negatively charged for better drug adsorption. ...
