Drug Targeting Organ-Specific Strategies

CL uptake (ml/min/g)
centration profiles are monitored (Figure 5.4a) [29]. Figure 5.3b shows the CL uptake for several
sugar-modified AVPs. It shows that the tissue-distribution profile largely depends on the
sugar moiety, and that glucose- (Glc), mannose- (Man) and 2dGlc-O-C8-AVP exhibit kidney-specific
distribution [23].
In the kidney, the CL uptake includes glomerular filtration as well as renal binding and
or uptake from the basal site. Hence, such CL uptake should give the apparent value
(CL uptake,app):
CL uptake,app = f pGFR + CL uptake,kidney
5.2 Renal Delivary Using Pro-Drugs 127
Figure 5.3. (a) Structure and (b) tissue uptake clearance of alkylglycoside-derivatized AVP. *Position
of 3 H-label. Adapted from reference [23].
(5.1)
where f p, GFR, and CL uptake,kidney represent respectively, the unbound plasma fraction, the
glomerular filtration rate, and the CL uptake value representing the unidirectional drug associ-