Evaluation of the Mucoadhesive Properties of Chitosan-Based Microstructured Lipid Carrier (CH-MLC)

Different mucoadhesive systems have been studied in recent years to increase the residence time of the delivery systems and to prolong the release of the drug. The aim of this work was to evaluate the mucoadhesive properties of chitosan-based Microstructured Lipid Carrier (CH-MLC) with a new approach which requires chitosan and mucin to be compacted into a tablet and mucoadhesion to be assessed on a non-mucoadhesive substrate.

This type of test showed that chitosan maintains a close bond with mucin even in the presence of a fluid and even encapsulated in microparticles. After this, using a bioreactor, the release of N-acetylcysteine (NAC) from the microparticles (NA-CH-MLC) through a layer of mucus mimicking the pathological conditions of a patient with cystic fibrosis was tested. The release of the active from NAC-CH-MLC demonstrated how the chitosan inside the microparticles acts as a penetration enhancer and how the microparticles can impart a prolonged release over time.

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Materials: Chitosan 90/100/A1 MW 86,000 g/mol, deacetylation degree 88–95%; Chitosan 90/400/A1 MW 300,000 g/mol, deacetylation degree 88–95%; and Chitosan 90/2000/A1 MW 1,323,000 g/mol, deacetylation degree 88–95%, were obtained by Kraeber & Co. GMBH, (Ellerberk, Germany). Mucin from porcine stomach Type II and Trehalose, diethylenetriaminepentaacetic acid (DTPA), sterile egg yolk and DNA (Sigma-Aldrich, Milan, Italy); sodium acetate trihydrate (Merck, Milan, Italy); acetic acid 96%, sodium chloride, magnesium stearate and Isooctane (Carlo Erba, Rodano, Italy); Caesalpinia spinosa gum (Solagum Tara™, Seppic, Milan, Italy); and glycerol dibehenate (Compritol 888 pastilles, Gattefossé, Milan, Italy) were obtained. Kolliphor P 407, a mix of polyoxyethylene (73%) and polyoxypropylene (POE–POP), was obtained from BASF (Ludwigshafen, Germany). Polyglyceryl-4 sorbitan olivate phosphate (Caldic, Milano, Italy), essential and non-essential L- amino acids (A.C.E.F., Piacenza, Italy) and Tryptone Soya Broth (Oxoid, Basingstoke, UK) were also obtained.

Article information: Guerini, M.; Condrò, G.; Perugini, P. Evaluation of the Mucoadhesive Properties of Chitosan-Based Microstructured Lipid Carrier (CH-MLC). Pharmaceutics 2022, 14, 170. https://doi.org/10.3390/pharmaceutics14010170