Chitosans for enhanced delivery of therapeutic peptides across intestinal epithelia: in vitro evaluation in Caco-2 cell monolayers

Nanoparticles Based on Chitosan Derivatives

“…Therefore the primary amino groups of its repeating units have been quaternized to bestow fixed, pH-independent positive charges on the polymer, thus making it soluble and active as an absorption promoter at physiological pH. In fact, TMC was found to act as an enhancer of drug, peptide and protein permeability across intestinal, nasal, buccal, ocular epithelium [47,[58][59][60][61][62][63][64][65][66]. TMC was shown to promote not only paracellular but also transcellular drug absorption [66].…”

“…Chitosan has been found to open the tight junctions connecting epithelial cells, through an interaction of its positively charged amino groups with negatively charged sites in the tight junctions, thereby promoting paracellular transepithelial absorption of drugs, peptides and proteins [10,[46][47][48][49][50][51][52][53][54][55][56][57]. The major drawback of unmodified chitosan as an absorption promoter is its insolubility at physiological neutral pH.…”

Oral absorption enhancement of salmon calcitonin by using bothN-trimethyl chitosan chloride and oligoarginines-modified liposomes as the carriers

“…However, the appearance of TMC resulted in dramatically prolonging the duration of validity. On the one hand, although TMC is considered to be of minor enzyme inhibition compared with other well-known enzyme inhibitors such as carbomer and polycarbophil (Kotzé et al, 1997), modification of TMC on the surface of liposomes could act as hydrophilic shell to prevent degradation from proteolytic enzymes; on the other hand, the absorption enhancing properties by opening the tight junction and mucoadhesive properties by interpenetrating into the mucus layer of TMC also played an important role in improving the oral absorption of calcitonin. Comparison of the AAC values can provide a quantitative evaluation of the therapeutic efficiency of the different formulations with regard to reduction in blood calcemia.…”

Dissolution and Permeation Properties of Naproxen From Solid-State Systems With Chitosan

“…Cells were seeded at a density of 10 2 cells/cm 2 on tissue culturetreated polycarbonate filters (area 1.13 cm 2 ) in Costar Snapwell six-well plates (Costar Europe Ltd, Badhoevedorp, The Netherlands). Filters were used for transport studies 21-28 days after seeding (Kotzé et al 1997).…”