The mechanism for increasing the oral bioavailability of poorly water-soluble drugs using uniform mesoporous carbon spheres as a carrier

Abstract

Uniform mesoporous carbon spheres (UMCS) were used as a carrier to improve the bioavailability of the model drug, celecoxib (CEL). Furthermore, we investigated the mechanism responsible for the improved bioavailability of CEL. The association, adhesion and uptake of UMCS by intestinal epithelial cells were studied by transmission electron microscopy (TEM), fluorescence-activated cell sorting (FACS) and laser confocal scanning microscopy (LCSM). UMCS was found to promote cellular uptake of CEL. Drug transport in Caco-2 cell monolayers proved that UMCS can significantly reduce the rate of drug efflux and improve CEL permeability. The dissolution rate of CEL from drug-loaded samples was markedly improved compared with pure crystalline CEL; moreover, oral bioavailability of CEL loaded into UMCS was also markedly improved compared with that of commercially available capsules. UMCS indicates the advantages and potential of this method to achieve improved oral absorption by increasing the dissolution rate, cellular uptake and permeability of the drug.

Mesoporous carbon nanomaterials in drug delivery and biomedical application

“…The permeability experiment was further conducted to investigate the mechanism underlying the absorption improvement by Wang et al. ( 2016 ). They recently reported the mechanism of uniform mesoporous carbon spheres (UMCS) used as a carrier to improve the bioavailability of insoluble drug celecoxib (CEL).…”

Nanostructured lipid carriers, solid lipid nanoparticles, and polymeric nanoparticles: which kind of drug delivery system is better for glioblastoma chemotherapy?

“…The surface morphology of T-PNPs, T-SLNs, and T-NLCs was investigated using transmission electron microscopy (TEM, JEM-1400; JEOL Ltd., Tokyo, Japan) (Wang et al, 2016). Three samples for testing were prepared, respectively, by placing a drop of nanoparticle suspension onto a copper grid and air drying, followed by negative staining with one drop of 3% aqueous solution of sodium phosphotungstate for contrast enhancement.…”

In Vitro Evaluation of Self-Nano-Emulsifying Drug Delivery Systems (SNEDDS) Containing Room Temperature Ionic Liquids (RTILs) for the Oral Delivery of Amphotericin B

“…The cellular uptake and intracellular distribution of coumarin-6 in Caco-2 cells was investigated by CLSM after cell exposure to SNEDDS and SNEDDS:RTILs. The white arrow in Figure 8 a shows that, upon incubation with Caco-2 monolayers, the coumarin-6 solution (control) is located close to the cytoplasm [ 39 , 40 ]. Images of SNEDDS containing coumarin-6, shown as green spots closely located to the nuclei and illustrated with a white arrow, are shown in Figure 8 b.…”