Renal Targeting: Peptide-Based Drug Delivery to Proximal
Tubule Cells
Version 2 2016-04-14, 12:56
Version 1 2016-03-30, 15:23
Posted on 2016-03-21 - 00:00
Kidney-specific drug targeting is
an attractive strategy to reduce
unwanted side effects and to enhance drug efficacy within the renal
tissue. For this purpose a novel kidney-specific drug carrier was
developed. The peptide sequence (KKEEE)3K triggers exceptional
renal specificity at high accumulation rates. Micro-PET imaging studies
of megalin-deficient mice indicate that the cellular endocytosis of
this carrier is mediated by megalin. This assumption is supported
by immunohistochemical analysis of FITC-labeled carrier peptide, which
exclusively accumulated at the apical side of proximal tubule cells
within the renal cortex. Scintigraphic studies of modified ciprofloxacin
conjugated to (KKEEE)3K confirmed the excellent drug targeting
potential of the peptide carrier. The conjugate accumulated entirely
in the kidneys, revealing flawless redirection of ciprofloxacin, a
compound that is mainly excreted by the liver. In conclusion, these
results suggest the potential of (KKEEE)3K as a promising
candidate for kidney-targeted drug delivery to proximal tubule cells.
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Wischnjow, Artjom; Sarko, Dikran; Janzer, Maria; Kaufman, Christina; Beijer, Barbro; Brings, Sebastian; et al. (2016). Renal Targeting: Peptide-Based Drug Delivery to Proximal
Tubule Cells. ACS Publications. Collection. https://doi.org/10.1021/acs.bioconjchem.6b00057
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AUTHORS (10)
AW
Artjom Wischnjow
DS
Dikran Sarko
MJ
Maria Janzer
CK
Christina Kaufman
BB
Barbro Beijer
SB
Sebastian Brings
UH
Uwe Haberkorn
GL
Gregor Larbig
AK
Armin Kübelbeck
WM
Walter Mier