In-vitro Cellular Uptake and Transport Study of 9-Nitrocamptothecin PLGA Nanoparticles Across Caco-2 Cell Monolayer Model

The uptake and transport of 9-nitrocamptothecin (9-nc), a potent anticancer agent, across caco-2 cell monolayers was studied as a free and plga nanoparticle loaded drug. different sizes (110 to 950 nm) of 9-nitrocamptothecin nanoparticles using poly (lactic-glycolic acid) were prepared by via the nanoprecipitation method. the transport of nanoparticles across the caco-2 cell monolayer as a function of incubation time and concentration was evaluated for each different nanoparticle formulation. the amount of 9-nc transported from the apical to the basolateral side and the uptake of the drug into the cells was determined by hplc. the uptake of intact nanoparticles into caco-2 cells was visualized by confocal laser scanning microscopy using 6-coumarin as a fluorescent marker. the study demonstrated that caco-2 cell uptake and transport of encapsulated 9-nitrocamptothecin is significantly affected by the diameter of the carrier and incubation time. in addition it was shown to be independent of concentration. the results indicated a significant accumulation of the drug in the cell membrane and an enhanced diffusion across the cell membrane. there was also a sustained release of characteristics pertaining to polymeric carriers that provided prolonged drug availability for absorptive cells.