Methods for Assessing Mucoadhesion: The Experience of an Integrative Approach

Yakubov, Gleb E.; Singleton, Scott; Williamson, Ann-Marie

doi:10.1002/9781118794203.ch09

Cited by 8 publications

(7 citation statements)

References 155 publications

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“…We presume that the Poloxamer ethoxylated groups that are in contact with the aqueous environment of the lamellar bilayer should interact with mucins through hydrogen bonds. In addition, the rate and the extension of the incorporation of bodily fluids are crucial factors that determine the retention of in situ gelling dosage forms (39). Then, we believe that this diffusion mechanism became more significant after addition of 100% SVF, which led to increased chemical interaction and a more rigid network.…”

Section: In Vitro Mucoadhesive Strength Testmentioning

confidence: 95%

Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs

et al. 2019

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The vaginal mucosa is a very promising route for drug administration due to its high permeability and the possibility to bypass first pass metabolism; however, current vaginal dosage forms present low retention times due to their dilution in vaginal fluids, which hampers the efficacy of many pharmacological treatments. In order to overcome these problems, this study proposes to develop a mucoadhesive in situ gelling liquid crystalline precursor system composed of 30% of oleic acid and cholesterol (7:1), 40% of ethoxylated and propoxylated cetyl alcohol, and 30% of a dispersion of 16% Poloxamer 407. The effect of the dilution with simulated vaginal fluid (SVF) on this system was evaluated by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheological studies, texture profile analysis (TPA), mucoadhesion study, in vitro drug release test using hypericin (HYP) as drug model, and cytotoxicity assay. PLM and SAXS confirmed the formation of an isotropic system. After the addition of three different concentrations of SVF (30, 50, and 100%), the resultant formulations presented anisotropy and characteristics of viscous lamellar phases. Rheology shows that formulations with SVF behaved as a non-Newtonian fluid with suitable shear thinning for vaginal application. TPA and mucoadhesion assays indicated the formation of long-range ordered systems as the amount of SVF increases which may assist in the fixation of the formulation on the vaginal mucosa. The formulations were able to control about 75% of the released HYP demonstrating a sustained release profile. Finally, all formulations acted as safe vaginal drug delivery systems.

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Section: In Vitro Mucoadhesive Strength Testmentioning

confidence: 95%

Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs

et al. 2019

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“…The strength of adhesion to mucin or the mean residence time in mucus of a given polymer are often used as the decision variables for selecting an appropriate mucoadhesive polymer for a given mucosal surface . However, functionalizing particles for delivery with mucoadhesive polymers can yield highly variable performance.…”

Section: Polymers For Nanoparticle Designmentioning

confidence: 99%

“…Spectroscopic methods such as nuclear magnetic resonance (NMR) and Fourier transform infrared (FTIR) spectroscopy provide insight into molecular interactions. FTIR measures bond vibrations in the material and associated perturbations as a result of interactions with mucus . This technique has been used to probe chain interpenetration at a PAA/mucin interface to reveal insights into mucoadhesion .…”

Section: Strategies To Study Mucus-nanoparticle Interactionsmentioning

confidence: 99%

“…FTIR elucidates specific responses caused by interactions with mucus, but peak convolution and spectral complexity lead to challenges in data interpretation. Similarly, NMR uses magnetic excitation to monitor interactions between different species in solution and generally encounters the same challenges as FTIR . Nevertheless NMR-based methods continue to evolve, and some progress has been made in understanding polymer–mucin interactions using relaxometry, evolution of line width, and macromolecular saturation transfer …”

Section: Strategies To Study Mucus-nanoparticle Interactionsmentioning

confidence: 99%

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Untangling Mucosal Drug Delivery: Engineering, Designing, and Testing Nanoparticles to Overcome the Mucus Barrier

Watchorn

Clasky

Prakash

et al. 2022

ACS Biomater. Sci. Eng.

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Mucus is a complex viscoelastic gel and acts as a barrier covering much of the soft tissue in the human body. High vascularization and accessibility have motivated drug delivery to various mucosal surfaces; however, these benefits are hindered by the mucus layer. To overcome the mucus barrier, many nanomedicines have been developed, with the goal of improving the efficacy and bioavailability of drug payloads. Two major nanoparticle-based strategies have emerged to facilitate mucosal drug delivery, namely, mucoadhesion and mucopenetration. Generally, mucoadhesive nanoparticles promote interactions with mucus for immobilization and sustained drug release, whereas mucopenetrating nanoparticles diffuse through the mucus and enhance drug uptake. The choice of strategy depends on many factors pertaining to the structural and compositional characteristics of the target mucus and mucosa. While there have been promising results in preclinical studies, mucus−nanoparticle interactions remain poorly understood, thus limiting effective clinical translation. This article reviews nanomedicines designed with mucoadhesive or mucopenetrating properties for mucosal delivery, explores the influence of site-dependent physiological variation among mucosal surfaces on efficacy, transport, and bioavailability, and discusses the techniques and models used to investigate mucus−nanoparticle interactions. The effects of non-homeostatic perturbations on protein corona formation, mucus composition, and nanoparticle performance are discussed in the context of mucosal delivery. The complexity of the mucosal barrier necessitates consideration of the interplay between nanoparticle design, tissue-specific differences in mucus structure and composition, and homeostatic or disease-related changes to the mucus barrier to develop effective nanomedicines for mucosal delivery.

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“…For effective hydrophobic interaction to occur, it requires high energy and low sensitivity to the surrounding conditions. Thus, hydrophobic interaction is effective in gastric conditions where pH is very low and suppresses the electrostatic interactions [30].…”

mentioning

confidence: 99%

Mucoadhesive Delivery System: A Smart Way to Improve Bioavailability of Nutraceuticals

Subramanian

2021

Foods

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The conventional oral administration of many nutraceuticals exhibits poor oral bioavailability due to the harsh gastric conditions and first-pass metabolism. Oral mucosa has been recognized as a potential site for the delivery of therapeutic compounds. The mucoadhesive formulation can adhere to the mucosal membrane through various interaction mechanisms and enhance the retention and permeability of bioactive compounds. Absorption of bioactive compounds from the mucosa can improve bioavailability, as this route bypasses the hepatic first-pass metabolism and transit through the gastrointestinal tract. The mucosal administration is convenient, simple to access, and reported for increasing the bioactive concentration in plasma. Many mucoadhesive polymers, emulsifiers, thickeners used for the pharmaceutical formulation are accepted in the food sector. Introducing mucoadhesive formulations specific to the nutraceutical sector will be a game-changer as we are still looking for different ways to improve the bioavailability of many bioactive compounds. This article describes the overview of buccal mucosa, the concept of mucoadhesion and related theories, and different techniques of mucoadhesive formulations. Finally, the classification of mucoadhesive polymers and the mucoadhesive systems designed for the effective delivery of bioactive compounds are presented.

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Methods for Assessing Mucoadhesion: The Experience of an Integrative Approach

Cited by 8 publications

References 155 publications

Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs

Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs

Untangling Mucosal Drug Delivery: Engineering, Designing, and Testing Nanoparticles to Overcome the Mucus Barrier

Mucoadhesive Delivery System: A Smart Way to Improve Bioavailability of Nutraceuticals

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