The Effect of Monomers and of Micellar and Vesicular Forms of Non-ionic Surfactants (Solulan C24 and Solulan 16) on Caco-2 Cell Monolayers

Abstract

Measurements of transepithelial electrical resistance (TEER), the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) test and monitoring of poly(ethylene glycol) (PEG) transport have been used to study the effects of the non-ionic surfactants Solulan C24 and Solulan 16, either free in solution or as an integral part of niosome bi-layers, on intestinal epithelial cells from man (Caco-2 cell monolayers). The effects on epithelial integrity and on the transport of the hydrophilic drug metformin depend on the concentration of the surfactants. At concentrations above 1% the effect on TEER of the surfactant in niosomal form and free in solution were equivalent whereas cell viability was preserved to a higher concentration of Solulans when the Solulans were present in the niosomal form. It was concluded that the toxic effect of niosomes arises from free surfactant present in the niosome suspension.

Colloidal Drug Formulations Can Explain “Bell-Shaped” Concentration–Response Curves

“…Conversely, above each surfactants’ CMC, these effects are removed; cell cultures show negligible permeability 48 and negligible toxicity. 49 …”

Effect of Charged and Non-ionic Membrane Additives on Physicochemical Properties and Stability of Niosomes

“…Normally, the charged molecule is added in niosomal formulation in an amount of 2.5-5 mol% because the high concentration of charged molecules can inhibit the formation of niosomes (9). The other additive is non-ionic substances in which cholesteryl poly-24-oxyethylene ether (SC24) is one of the widely used non-ionic surfactants (10). It is added in niosomal formulations at the range of 5-10 mol% to provide the steric barrier to vesicle membrane, which prevents vesicle aggregation and leads to enhance of physical stability of niosomes (11).…”

Polyamine Aza-Cyclic Compounds Demonstrate Anti-Proliferative Activity In Vitro But Fail to Control Tumour Growth In Vivo

“…We also directly compared the haemolytic potential of these compounds with that of the poly(propylenimine) dendrimer (DAB 16) which has shown good in vivo anti-proliferative activity with little signs of toxicity at tumouricidal doses: DAB16 was more haemolytic than both hexacyclen and CL4. 15 It appears that haemolysis involves a crucial kinetic component in which a sufficient number of individual amine molecules must associate with the erythrocyte surface within a finite period of time. 2).…”