Kidney targeted delivery of asiatic acid using a FITC labeled renal tubular-targeting peptide modified PLGA-PEG system

[Display omitted] Chronic kidney disease (CKD) is one of the leading public health problems worldwide and finally progresses to end-stage renal disease. The therapeutic options of CKD are very limited. Thus, development of drug delivery systems specific-targeting to kidney may offer more options. Here we developed an efficient kidney-targeted drug delivery system using a FITC labeled renal tubular-targeting peptide modified PLGA-PEG nanoparticles and investigated the intrarenal distribution and cell-type binding. We found that the modified nanoparticles with an approximate diameter of 200 nm exhibited the highest binding capacity with HK-2 cells and fluorescence and immunohistochemical analysis showed they mainly localized in renal proximal tubules by passing through the basolateral side. Furthermore, these kidney-specific nanoparticles could significantly enhance the therapeutic effects of asiatic acid, an insoluble triterpenoid compound as drug delivery carriers. In conclusion, these results suggest the potential of the peptide modified PLGA-PEG nanoparticles as kidneytargeted drug delivery system to proximal tubular cells in treatment of CKD.