Quantitative evaluation of mucoadhesive polymers to compare the mucoadhesion

Lee, Cho-A; Kim, Bo-Sik; Cho, Cheong-Weon

doi:10.1007/s40005-016-0233-4

Cited by 11 publications

(6 citation statements)

References 42 publications

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“…The negative charge of mucin particles can be explained by the presence of sialic acid residues, i.e., oligosaccharide chains that contain a large number of carboxyl and sulfate groups [ 96 ]. After mixing the mucin dispersion with chitosan-containing solutions, the zeta potential changed from negative to positive values (21 mV) due to the presence of protonated amino groups of chitosan [ 101 , 133 ]. On the other hand, when adding the solution with hyaluronate to the mucin dispersion, the negative value of the zeta potential increases significantly (−25 mV), and this increase in zeta potential is explained by the anionic nature of hyaluronate and the presence of a large number of carboxyl groups in the structure of this polymer.…”

Section: Characterization Of Mucoadhesive Ophthalmic Preparationsmentioning

confidence: 99%

Biopolymers in Mucoadhesive Eye Drops for Treatment of Dry Eye and Allergic Conditions: Application and Perspectives

Račić

Krajišnik

2023

Pharmaceutics

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Dry eye syndrome and allergic conjunctivitis are the most common inflammatory disorders of the eye surface. Although eye drops are the most usual prescribed dosage form, they are characterized by low ocular availability due to numerous barrier mechanisms of the eye. The use of biopolymers in liquid ophthalmic preparations has numerous advantages, such as increasing the viscosity of the tear film, exhibiting bioadhesive properties, and resisting the drainage system, leading to prolonged retention of the preparation at the site of application, and improvement of the therapeutic effect. Some mucoadhesive polymers are multifunctional excipients, so they act by different mechanisms on increasing the permeability of the cornea. Additionally, many hydrophilic biopolymers can also represent the active substances in artificial tear preparations, due to their lubrication and moisturizing effect. With the modification of conventional ophthalmic preparations, there is a need for development of new methods for their characterization. Numerous methods for the assessment of mucoadhesiveness have been suggested by the literature. This review gives an overview related to the development of mucoadhesive liquid ophthalmic formulations for the treatment of dry eye and allergic conditions.

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Section: Characterization Of Mucoadhesive Ophthalmic Preparationsmentioning

confidence: 99%

Biopolymers in Mucoadhesive Eye Drops for Treatment of Dry Eye and Allergic Conditions: Application and Perspectives

Račić

Krajišnik

2023

Pharmaceutics

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“…The mucoadhesiveness of Fas/PL-Lipo disp , Fas/PL-Lipo P407 gel , Fas/PL-Lipo P407/HPMC gel and B-Lipo P407/HPMC gel was indirectly assessed by measuring the changes in viscosity following incubation with mucin. 38 Mucin 20% w/v was first hydrated with distilled water, then gently stirred at room temperature for complete dispersion. Formulations were incubated with hydrated mucin in a 2:1 ratio, under continuous magnetic stirring at room temperature for 15 minutes.…”

Section: In Vitro Mucoadhesion Studymentioning

confidence: 99%

Exploring a Novel Fasudil-Phospholipid Complex Formulated as Liposomal Thermosensitive in situ Gel for Glaucoma

Khallaf¹,

El‐Moslemany²,

Ahmed

et al. 2022

IJN

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Purpose: Fasudil hydrochloride (Fas), a rho-associated protein kinase inhibitor, proved to be promising for glaucoma management owing to its IOP lowering and antioxidant effects. However, its highly hydrophilic nature limits ocular permeation and bioavailability. Hence, the study objective was the development of Fas loaded vesicular system with high entrapment efficiency formulated as a thermosensitive gel for local administration aiming to enhance ocular retention and permeation and hence therapeutic efficacy. Methods: Fasudil complex with phospholipid (Fas/PL) was prepared by solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FT-IR) and X-ray diffraction (XRD). Fas/PL was further formulated as liposomes by methanol injection method and characterized regarding colloidal properties, entrapment efficiency (EE%) and in vitro drug release. The prepared liposomes were incorporated into an optimized thermosensitive in situ gel (Fas/PL-Lipo P407/HPMCgel ) selected based on gelling time and temperature and rheological properties. The effect of incorporation into gel on the in vitro characteristics of liposomes was investigated. The in vitro mucoadhesive potential, ex vivo permeation, irritability and efficacy in a glaucoma rabbit model were also assessed. Results: FT-IR and XRD suggested interactions between Fas and PL, proposing complexation. Fas/PL liposomal dispersions showed good colloidal properties (particle size: 132.5 ± 1.6 nm, zeta potential: −21.6 ± 0.9 and %EE 78.6 ± 0.3%) with sustained drug release. In situ thermosensitive gel (20% poloxamer 407 and 0.5% HPMC) showed optimum gelling properties. The selected gel formulation reduced burst release of the drug, enhanced mucoadhesive properties and prolonged corneal permeation ex vivo. HET-CAM test confirmed that the prepared formulations were non-irritant. In vivo pharmacodynamic study indicated improved bioavailability and significantly lower intraocular pressure (IOP) of Fas/PL-Lipo P407/HPMC gel compared to drug solution and liposomal dispersion. Conclusion:The results present Fas/PL-Lipo P407/HPMC gel as a potential platform for ophthalmic delivery of fasudil with improved pharmaceutical attributes and enhanced bioavailability and efficacy in glaucoma.

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“…However, these interactions depend significantly on the protonation state of the functional groups of the polymer, which are closely related to the pH [87]. Consequently, the more acidic the environment is during the interaction, the higher degree of protonation on their surface the chitosan:TPP nanoparticles exhibit, which allows a greater number of interactions with the negatively charged mucosal compounds through the formation of polyelectrolyte complexes that enhance adhesion [88,89], as Figure 5a-c shows. Nevertheless, under neutral or alkaline pH conditions, the amino groups deprotonate, and the positive charges of chitosan are neutralized, forming an insoluble biopolymer layer that tends to precipitate, limiting its mucoadhesive properties [84,90,91], as Figure 5d the two biopolymers that influence an entanglement of mucin and polymer chains [82], causing the formation of a resulting polymeric network with an enhanced elastic modulus (G′) in comparison with the sum of the elastic modulus (G′) values of the single components [83].…”

Section: Assessment Of Chitosan Nanoparticles-mucus Interaction Throu...mentioning

confidence: 99%

“…However, these interactions depend significantly on the protonation state of the functional groups of the polymer, which are closely related to the pH [87]. Consequently, the more acidic the environment is during the interaction, the higher degree of protonation on their surface the chitosan:TPP nanoparticles exhibit, which allows a greater number of interactions with the negatively charged mucosal compounds through the formation of polyelectrolyte complexes that enhance adhesion [88,89], as Additionally, a viscosity-based synergistic approach can be taken to determine rheological synergism (∆ η) based on the difference between the viscosity of the mixture and the sum of the individual components [87]. The viscosity synergism of a molecular dispersion of a fully hydrated polymer and mucin can be considered a reflection of the mucoadhesive strength of the polymer-mucin system [92] because the chain entanglement and molecular bonding among the mucin and the mucoadhesive polymer alter the rheological behavior of both materials [80].…”

Section: Assessment Of Chitosan Nanoparticles-mucus Interaction Throu...mentioning

confidence: 99%

Triborheological Analysis of Reconstituted Gastrointestinal Mucus/Chitosan:TPP Nanoparticles System to Study Mucoadhesion Phenomenon under Different pH Conditions

et al. 2022

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Polymeric nanoparticles have attracted much attention as pharmaceutical delivery vehicles to prolong residence time and enhance the bioavailability of therapeutic molecules through the mucoadhesive phenomenon. In this study, chitosan:TPP nanoparticles were synthetized using the ionic gelation technique to analyze their mucoadhesive interaction with reconstituted porcine gastrointestinal mucus from a triborheological point of view under different pH conditions (pH = 2.0, 4.0, 6.0 and 7.0). The triborheological profile of the reconstituted mucus was evaluated at different pH environments through the oscillation frequency and the flow sweep tests, demonstrating that the reconstituted mucus exhibits shear thinning behavior regardless of pH, while its viscoelastic properties showed a change in behavior from a polymeric solution performance under neutral pH conditions to a viscoelastic gel under acidic conditions. Additionally, a rheological synergism analysis was performed to visualize the changes that occur in the viscoelastic properties, the viscosity and the coefficient of friction of the reconstituted mucus samples as a consequence of the interaction with the chitosan:TPP nanoparticles to determine or to discard the presence of the mucoadhesion phenomenon under the different pH values. Mucoadhesiveness evaluation revealed that chitosan:TPP exhibited strong mucoadhesion under highly acidic pH conditions, below its pKa value of 6.5. In contrast, at neutral conditions or close to its pKa value, the chitosan:TPP nanoparticles’ mucoadhesiveness was negligible.

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Quantitative evaluation of mucoadhesive polymers to compare the mucoadhesion

Cited by 11 publications

References 42 publications

Biopolymers in Mucoadhesive Eye Drops for Treatment of Dry Eye and Allergic Conditions: Application and Perspectives

Biopolymers in Mucoadhesive Eye Drops for Treatment of Dry Eye and Allergic Conditions: Application and Perspectives

Exploring a Novel Fasudil-Phospholipid Complex Formulated as Liposomal Thermosensitive in situ Gel for Glaucoma

Triborheological Analysis of Reconstituted Gastrointestinal Mucus/Chitosan:TPP Nanoparticles System to Study Mucoadhesion Phenomenon under Different pH Conditions

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