In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers

Lehr, Claus‐Michael; Bouwstra, Joke A.; Schacht, Etienne; Junginger, Hans E.

doi:10.1016/0378-5173(92)90353-4

Cited by 920 publications

(441 citation statements)

References 5 publications

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“…The main contribution towards the interaction is clearly electrostatic, with some hydrophobic contribution [7]. The AFM data also support the macroscopic tensiometric measurements [9]. This demonstration should assist with the design of more efficient gastrointestinal drug delivery systems [30,31].…”

Section: Resultssupporting

confidence: 70%

“…As has been previously indicated [7,19,20,29] a significant interaction has been shown between the purified PGM and this form of chitosan on the basis of molecular hydrodynamics, electron microscopy and scanning tunnelling microscopy, consistent with macroscopic tensiometry studies [9]. Figure 4 illustrates the complex formed between the chitosan and mucin structures when mixed together in solution and then immobilized to the APTES-coated substrate.…”

Section: Complexes Of Pgm and Chitosan At 01 M Ionic Strengthsupporting

confidence: 82%

“…Interactions with mucin appear to be both electrostatic, via NH $ + groups on the chitosan with either COO − or SO $ − groups on the mucin carbohydrate side chains, and\or hydrophobic, via kCH $ groups on acetylated chitosan residues with kCH $ groups on mucin side chains [depending on the degree of acetylation of the chitosan, local solvent conditions (pH, ionic strength) and the degree of sulphonation and sialic acid content of the mucin]. These molecular studies have been supported by macroscopic studies involving mechanical measurements based around the tensiometry principle on whole mucus [9].…”

Section: Introductionmentioning

confidence: 99%

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Atomic force microscopy of gastric mucin and chitosan mucoadhesive systems

Deacon

McGurk

Roberts

et al. 2000

Biochemical Journal

118

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Atomic force microscopy has been utilized to probe, at a molecular level, the interaction between purified pig gastric mucin (PGM) and a mucoadhesive cationic polymer, chitosan (sea cure 210j), with a low degree (approx. 11 %) of acetylation. Images were produced detailing the structures of both PGM and chitosan in 0.1 M acetate buffer (pH 4.5), followed by the complex of the two structures in the same buffer. PGM in 0.1 M acetate buffer revealed long linear filamentous structures, consistent with earlier electron microscopy and scanning tunnelling micoscopy studies. The chitosan molecules also adopted a linear conformation in the same buffer, although with a smaller average

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Section: Resultssupporting

confidence: 70%

Section: Complexes Of Pgm and Chitosan At 01 M Ionic Strengthsupporting

confidence: 82%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Atomic force microscopy of gastric mucin and chitosan mucoadhesive systems

Deacon

McGurk

Roberts

et al. 2000

Biochemical Journal

118

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“…In recent years, the most frequently explored polysaccharide for the design of nanodelivery systems was chitosan, a cationic polymer composed of repeating β-(1,4)-linked N-acetylglucosamine and D-glucosamine units, which is obtained by chitin deacetylation and assumes different molecular weights and deacetylation degrees (Chiellini et al, 2008;Hassani et al, 2012;Mizrahy and Peer, 2012). Apart from the reported biocompatibility and biodegradability (Dornish et al, 1997;Grenha et al, 2010a;Hirano et al, 1988), the most outstanding properties of chitosan rely on its mucoadhesive character (Lehr et al, 1992) and demonstrated ability to potentiate transmucosal absorption both as molecule (Artursson et al, 1994;Borchard et al, 1996;Portero et al, 2002) and in the form of nanoparticle (Al-Qadi et al, 2012;De Campos et al, 2001;Fernández-Urrusuno et al, 1999a;Prego et al, 2005a;Yamamoto et al, 2005).…”

Section: Introductionmentioning

confidence: 99%

Pullulan-based nanoparticles as carriers for transmucosal protein delivery

Dionísio

Cordeiro

Remuñán‐López

et al. 2013

European Journal of Pharmaceutical Sciences

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Polymeric nanoparticles have revealed very effective in transmucosal delivery of proteins. Polysaccharides are among the most used materials for the production of these carriers, owing to their structural flexibility and propensity to evidence biocompatibility and biodegradability. In parallel, there is a preference for the use of mild methods for their production, in order to prevent protein degradation, ensure lower costs and easier procedures that enable scaling up.In this work we propose the production of pullulan-based nanoparticles by a mild method of polyelectrolyte complexation. As pullulan is a neutral polysaccharide, sulfated and aminated derivatives of the polymer were synthesized to provide pullulan with a charge. These derivatives were then complexed with chitosan and carrageenan, respectively, to produce the nanocarriers. Positively charged nanoparticles of 180-270 nm were obtained, evidencing ability to associate bovine serum albumin, which was selected as model protein. In PBS pH 7.4, pullulan-based nanoparticles were found to have a burst release of 30% of the protein, which maintained up to 24h. Nanoparticle size and zeta potential were preserved upon freeze-drying in the presence of appropriate cryoprotectants. A factorial design was approached to assess the cytotoxicity of raw materials and nanoparticles by the metabolic test MTT. Nanoparticles demonstrated to not cause overt toxicity in a respiratory cell model (Calu-3). Pullulan has, thus, demonstrated to hold potential for the production of nanoparticles with an application in protein delivery.

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“…Moreover, chitosan has the significant potential of reducing transepithelial electrical resistance and transiently opening tight conjunction between epithelial cells [9]. In addition, its mucoadhesive property [10] is another advantage for promoting drug adsorption due to combination with anionic substructures such as sialic acid moieties of the mucosa layer. The adhesion of chitosan at the site of drug absorption offers various advantages for an improved uptake of therapeutic peptides [11,12].…”

Section: Introductionmentioning

confidence: 99%

Development and characterization of new insulin containing polysaccharide nanoparticles

Sarmento

Ribeiro

Veiga

et al. 2006

Colloids and Surfaces B: Biointerfaces

230

140

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A nanoparticle insulin delivery system was prepared by complexation of dextran sulfate and chitosan in aqueous solution. Parameters of the formulation such as the final mass of polysaccharides, the mass ratio of the two polysaccharides, pH of polysaccharides solution, and insulin theorical loading were identified as the modulating factors of nanoparticle physical properties. Particles with a mean diameter of 500 nm and a zeta potential of approximately −15 mV were produced under optimal conditions of DS:chitosan mass ratio of 1.5:1 at pH 4.8. Nanoparticles showed spherical shape, uniform size and good shelf-life stability. Polysaccharides complexation was confirmed by differential scanning calorimetry and Fourier transformed infra-red spectroscopy. An association efficiency of 85% was obtained. Insulin release at pH below 5.2 was almost prevented up to 24 h and at pH 6.8 the release was characterized by a controlled profile. This suggests that release of insulin is ruled by a dissociation mechanism and DS/chitosan nanoparticles are pH-sensitive delivery systems. Furthermore, the released insulin entirely maintained its immunogenic bioactivity evaluated by ELISA, confirming that this new formulation shows promising properties towards the development of an oral delivery system for insulin.

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In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers

Cited by 920 publications

References 5 publications

Atomic force microscopy of gastric mucin and chitosan mucoadhesive systems

Atomic force microscopy of gastric mucin and chitosan mucoadhesive systems

Pullulan-based nanoparticles as carriers for transmucosal protein delivery

Development and characterization of new insulin containing polysaccharide nanoparticles

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