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

Abstract

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.

Evaluation of Physically and/or Chemically Modified Chitosan Hydrogels for Proficient Release of Insoluble Nystatin in Simulated Fluids

“…Thus, physically cross-linked chitosan hydrogel CS-NYSm showed increased inhibitory activity, mainly due to the presence of positively charged amino groups of CS and their interactions with the negatively charged fungal membrane. This mechanism of action by electrostatic attraction is known to induce damage to cell membranes [ 24 ]. However, chemically cross-linked CS hydrogels manifested antifungal activity close to those of physical gels, especially in the case of the CS-NYSm-SA/DS-2 hydrogel.…”

“…The abundant presence of functional groups (–NH 2 at C2 and –OH at C3 and C6) provides both chemical reactivity and bioactivity to the chitosan chains [ 23 ]. As for the latter, chitosan is well-known for possessing mucoadhesive properties, due to the strong electrostatic interaction between positively charged amino groups and negatively charged epithelial surfaces and sialic acid (component of mucus) [ 24 ].…”

Development of Lyophilised Eudragit® Retard Nanoparticles for the Sustained Release of Clozapine via Intranasal Administration

“…The difference (Δ Abs ) was taken as a measure of the interaction between mucin and NPs [ 22 ]. If Δ Abs ≤ 0, it means that there is no interaction; if Δ Abs > 0, a strong interaction between mucin and the NPs is envisaged [ 25 ]. The experiments were repeated in duplicate.…”

Chitosan-based hydrogels: From preparation to applications, a review

“…It is within this context that the amino groups effectively engage hydrogen atoms, evolving into ammonia ions (–NH 3 + ), before forming steadfast macromolecules that diligently neutralize the pernicious effects of free radicals. Similarly, chitosan's unparalleled antibacterial characteristics ( Guerini, Condro, & Perugini, 2022 ) result from electrostatic interactions between positively charged amino groups beautifully dispersed along its molecular chain and their negatively charged equivalents. This mesmerizing electrostatic attraction process instigates a cascade of damage to the cell membrane, unequivocally accounting for the observed antibacterial activity.…”