Whey protein mucoadhesive properties for oral drug delivery: Mucin–whey protein interaction and mucoadhesive bond strength

Hsein, Hassana; Garrait, Ghislain; Beyssac, Eric; Hoffart, Valérie

doi:10.1016/j.colsurfb.2015.10.016

Cited by 47 publications

(45 citation statements)

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“…Thus, the main secondary conformation of DWP-sp was antiparallel β-sheets characterized by unfolding and aggregation of proteins. This structure was similar to FTIR results obtained in our previous study on DWP powder obtained by polymeric solution freeze-drying [12] indicating that heat elements during spray-drying had no influence on DWP-sp structure.…”

Section: Ftirsupporting

confidence: 89%

“…This was due to unfolding of polymeric chains following denaturation, which expose functional groups such as free thiols and hydrophobic groups. Thiol functional groups are the main key for mucoadhesion because they allow establishment of covalent disulfide bonds between polymer and cysteines of the mucus [12]. By comparison with mucoadhesivity of hydrogel or microparticles made of DWP [12,57], these results effectively proved that the denaturation clearly exhibited these properties and the spray-drying technique turned to maintain them.…”

Section: Mucoadhesive Propertiesmentioning

confidence: 98%

“…The amount of free thiol in WP samples was determined spectrophotometrically with Ellman's reagent (Pierce Biotechnology, Rockford, USA) according to the manual instructions guide [12,22]. First, NWP-sp and DWP-sp powders were dissolved in deionized water (pH 6.8) at 20 mg.mL -1 and 250 μL of the obtained WP solutions were mixed with 2500 μL of reaction buffer and 50 μL of Ellman's reagent.…”

Section: Free Thiol Content Determinationmentioning

confidence: 99%

“…As expected, denaturation favored exposition of free thiol in both, solution and spray-dried powder forms. Unfolding of polymeric chains following denaturation was the main reason for the exponential increase in thiol groups [12] whereas rearrangement of functional groups during particle formation probably decreased accessible thiol groups following spray-drying. Rearrangement could be the reformation of aggregates by thiol-disulfide interchange [45] or the sharing of total free thiol groups between the surface and the core of particles.…”

Section: Free Thiol Determinationmentioning

confidence: 99%

“…These properties can contribute to the promotion of oral drug bioavailability, more specifically, bioavailability of drugs such as insulin; and this took place after administration of DWP microparticles to rats [9]. Indeed, compared to WP's native form, DWP are highly mucoadhesive [12], and in reticulated microparticle form, exhibited controlled release of encapsulated drugs, opened tight junctions, and inhibited proteolytic enzymatic activity [13]. However, denaturation is not without disadvantages.…”

Section: Introductionmentioning

confidence: 99%

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Atomization of denatured whey proteins as a novel and simple way to improve oral drug delivery system properties

Hsein

Garrait

Mumin

et al. 2017

International Journal of Biological Macromolecules

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In the sphere of drug delivery, denatured whey protein (DWP) has in recent times gained press. However, to date, no scalable and affordable dosage form has been developed. The objective of our study was to evaluate the potential use of spray-dried DWP as a ready to use excipient for oral drug delivery. Therefore, solid state, FTIR spectra and wettability were studied. Dissolution, mucoadhesion and the effect on paracellular permeability were also evaluated. The spray-dried DWP particles were spherical with 4μm mean diameter. Further, relative to native WP, the spray-dried DWP particles bore reduced wettability, and their structure was characterized by the exposure of a high amount of free thiol and by the formation of intermolecular β-sheets. The DWP powders were mucoadhesive, enzymatic inhibitors, biocompatible and they induced the opening of tight junctions. Our study shows great potential for the use of spray-drying as a technique to modify the dissolution rate of drugs and enhance the oral bioavailability of molecules. That is, the use of spray drying as a single step ready to use DWP excipient.

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Section: Ftirsupporting

confidence: 89%

Section: Mucoadhesive Propertiesmentioning

confidence: 98%

Section: Free Thiol Content Determinationmentioning

confidence: 99%

Section: Free Thiol Determinationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Atomization of denatured whey proteins as a novel and simple way to improve oral drug delivery system properties

Hsein

Garrait

Mumin

et al. 2017

International Journal of Biological Macromolecules

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Improved Gastric Acid Resistance and Adhesive Colonization of Probiotics by Mucoadhesive and Intestinal Targeted Konjac Glucomannan Microspheres

Liu

et al. 2020

Adv Funct Materials

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The low survival rate in harsh stomach conditions and short retention in intestine of probiotics greatly limit their health benefits. To solve this problem, thiolated oxidized konjac glucomannan (sOKGM) microspheres is designed with pH responsive and mucoadhesive properties. First, an increased survival rate of probiotics by sOKGM microspheres encapsulation in simulated gastric fluid (SGF) is discovered in contrast to the zero‐survival rate of naked probiotics. sOKGM/probiotics even show a higher survival rate in SGF compared with commercial Bb12 formulation. Further, an enhanced mucoadhesion of probiotics to intestinal mucus by mediated interactions with sOKGM is confirmed by isotherm titration calorimetry, rheology, and tensile measurements. The in vivo intestinal transition experiment indicates a prolonged retention of probiotics at intestine by sOKGM encapsulation. Moreover, in vivo evaluation of enhanced colonization and proliferation by sOKGM/probiotics is demonstrated by the fecal and intestinal bacteria copy number via quantitative polymerase chain reaction (qPCR) detection. Further investigation of the alleviation of constipation by sOKGM containing Bifidobacterium animalis subsp. lactis A6 suggests that sOKGM increases the abundance of Bifidobacterium, balanced intestinal flora, and alleviated constipation in mice compared with other formulations. sOKGM with both enhanced gastric acid resistance and adhesion colonization at intestine can effectively improve the function of probiotics.

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Study of Lactobacillus plantarum coated with Tremella polysaccharides to improve its intestinal adhesion

Zhu,

Tang,

Wang

et al. 2024

J Sci Food Agric

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BackgroundThe adhesion of probiotics to the intestine is crucial to their probiotic function. Tremella polysaccharides (TPS) (with sodium casein) have shown the potential in previous studies to encapsulate probiotics and protect them in the simulated gastrointestinal tract. This paper further explored the effect of TPS (with sodium casein) on the adhesion of probiotics.ResultsLactobacillus plantarum was coated in different proportions in TPS and sodium casein and then freeze‐drying. The rheological properties of the mixture of probiotics powder and mucin solution were determined by static and dynamic rheological analysis. Aqueous solutions of probiotics powder and mucin mixture exhibited pseudoplastic fluid rheological properties. The higher the proportion of TPS content, the higher the apparent viscosity and yield stress. The mixed bacterial powder and mucin fluid displayed certain thixotropy and obeyed the Herschel‐Bulkley model. It indicated that TPS increased the bio‐adhesive force of probiotics powder and mucin. When using TPS as the only carbon source, the adhesion of L. plantarum to Caco‐2 cells increased by 228% compared to glucose in vitro. In addition, 12 proteins with adhesion function were detected in the whole‐cell proteome of L. plantarum. Among them, 10 proteins with adhesion function were abundant when grown with TPS as a carbon source.ConclusionTherefore, TPS possess prebiotic properties and can promote the intestinal adhesion of L. plantarum.This article is protected by copyright. All rights reserved.

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Whey protein mucoadhesive properties for oral drug delivery: Mucin–whey protein interaction and mucoadhesive bond strength

Cited by 47 publications

References 46 publications

Atomization of denatured whey proteins as a novel and simple way to improve oral drug delivery system properties

Atomization of denatured whey proteins as a novel and simple way to improve oral drug delivery system properties

Improved Gastric Acid Resistance and Adhesive Colonization of Probiotics by Mucoadhesive and Intestinal Targeted Konjac Glucomannan Microspheres

Study of Lactobacillus plantarum coated with Tremella polysaccharides to improve its intestinal adhesion

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