An in vitro study of mucoadhesion and biocompatibility of polymer coated liposomes on HT29-MTX mucus-producing cells

Abstract

Drug delivery to the oral cavity poses a significant challenge due to the short residence time of the formulations at the site of action. From this point of view, nanoparticulate drug delivery systems with ability to adhere to the oral mucosa are advantageous as they could increase the effectiveness of the therapy. Positively, negatively and neutrally charged liposomes were coated with four different types of polymers: alginate, low-ester pectin, chitosan and hydrophobically modified ethyl hydroxyethyl cellulose. The mucoadhesion was studied using a novel in vitro method allowing the liposomes to interact with a mucus-producing confluent HT29-MTX cell-line without applying any external force. MTT viability and paracellular permeability tests were conducted on the same cell-line. The alginate-coated liposomes achieved a high specific (genuine) mucin interaction, with a low potential of cell-irritation. The positively charged uncoated liposomes achieved the highest initial mucoadhesion, but also displayed a higher probability of cell-irritation. The chitosan-coated liposomes displayed the highest potential for long lasting mucoadhesion, but with the drawback of a higher general adhesion (tack) and a higher potential for irritating the cells.

Innovative Methods and Applications in Mucoadhesion Research

“…Chen et al evaluated the mucoadhesion of probiotic alginate microcapsules by counting Lactobacillus reuteri strain released from the capsules adhering to the HT29‐MTX after 1 h of incubation . In another study, mucoadhesion of fluorescently labeled, noncoated and polymer‐coated liposomes was measured after 2 h of incubation with HT29‐MTX cell monolayer . The amount of liposomes adhering to the mucus was determined by measuring the fluorescence intensity both directly on the cell monolayer and indirectly from the supernatant solution after incubation.…”

“…Different studies have revealed positively charged materials such as chitosan and positively charged lipids to exert the highest mucoadhesive/bioadhesive properties in the oral cavity . However, toxicity studies have shown that positively charged formulations seem to be more toxic than their negative counterparts .…”

Protein-Based Structures for Food Applications: From Macro to Nanoscale

“…In order to answer these challenges, protein-based structures (e.g., hydrogels) are being developed at macro-(≥1,000 µm) and microscale (0.1-1,000 µm) and used to encapsulate, protect, and release bioactive compounds to a specific target. The design of a structure, namely its size, is highly important once it was observed that micro-and nanoscale structures are favorable for encapsulation properties Permeability enhancer High permeability in contact with cells High water-holding capacity Verheul and Roefs, 1998;Cooksey et al, 1999;Sobral et al, 2001;Rhim et al, 2007;Neethirajan and Jayas, 2011;Adamczak et al, 2016 Viscosity Low effect on viscosity Promote the development of semi-solid behavior Akkermans et al, 2007;Bokkhim et al, 2013;Muschiolik and Dickinson, 2017 Solubility Improved solubility, targetability, and adhesion to tissues…”

Development and in�vitro evaluation of mucoadhesive patches of methotrexate for targeted delivery in oral cancer

“…Mucoadhesive buccal patches offered benefits compared with conventional methods (10). Due to the short residence time of oral gels in oral cavity, buccal patches have advantages of increased residence time and drug release (5).…”