Janus microspheres for enhanced enteral drug delivery: Preparation and orientated attachment to a Caco-2 monolayer

Targeting cellular gaps using Janus nanoparticles containing cationic polymers and surfactant lipids

“…Janus and non-Janus particles were added to Caco-2 cell monolayers. When the nanoparticles were added to the apical side of the Caco-2 monolayer at 4 mg/mL, as previously reported (20), fragmentation of the cell nuclei was observed. Therefore, subsequent nanoparticle incubation experiments were performed at a concentration of 0.4 mg/mL.…”

“…However, because the lipids and cells used in lipid nanoparticles and their incubation time with cells in this study differed from those in the previous report, further research is required to accurately determine the cytotoxicity of the Janus and non-Janus nanoparticles we used. As a result, unlike the Janus microparticles reported previously (average particle size: 30 μm) (20), the Janus nanoparticles of all formulations were taken up by Caco-2 cells. One of the reasons why all nanoparticles were incorporated into the cells could be because of their small particle size, which is known to influence cellular uptake (6,7).…”

“…In this study, the appropriate solvent removal rate was obtained from the volume of the water phase to that of methylene chloride. To this end, we fixed 100 mL as the volume of the water phase in the solvent evaporation process, which provided approximately 1.5 times the saturated solubility (1.3 g/100 mL at 20℃) for the methylene chloride applied in our previous study (20).…”

“…Regarding the orientation of attached particles on a membrane, it has been reported that hollow microtubes can be formed by designing two biologically distinguishable regions: one exhibiting high binding affinity for cells and the other being essentially resistant to cell binding (26). In our previous study, orientational attachment on the human Caucasian colon adenocarcinoma (Caco-2) cell membrane was confirmed using Janus-type microspheres composed of a cationic polymer and hard fat (20). We found that the Janus microspheres had unique orientation properties in that the cationic side was in contact with the surface of the Caco-2 cell membrane while the lipid side faced the gastrointestinal lumen.…”

“…Hence, these particles can encapsulate specific drugs with different properties in distinct domains or independently release each drug after a different trigger, such as heat (18) and light (19). We reported that both hydrophobic and hydrophilic fluorescent substances could be encapsulated into Janus microspheres (20). Janus particles can also have separate functions in their distinct domains, including drug-loading and targeting domains.…”