In-vitro cellular uptake and transport study of 9-nitrocamptothecin PLGA nanoparticles across Caco-2 cell monolayer model

Document Type: Research article

Authors

1 Department of Pharmaceutics, School of Pharmacy, University of Florida, Gainesville, USA

2 Department of Pharmaceutics, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran, IRAN

3 Department of Pharmaceutics, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran. Department of Pharmaceutics, School of Pharmacy, Florida, Gainesville, USA. University of Medical.

Abstract

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.

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