Drug targeting to the liver with bile acids: THE “trojan horse” resurrected?
Dirk K. F. Meijer – 1 May 1993 – Bile acids are selectively taken up from portal blood into the liver by specific transport systems in the hepatocyte plasma membrane. Therefore, studies were performed to evaluate the potential of bile acids as shuttles to deliver drugs specifically to the liver. The alkylating cytostatic drug chlorambucii and the fluorescent prolyl‐4‐hydroxylase inhibitor 4‐nitrobenzo‐2‐oxa‐1,3‐diazol‐β‐Ala‐Phe‐5‐oxaproline‐Gly were covalently linked via an amide bond to 7α, 12α,‐dihydroxy‐3β‐(ω‐aminoalkoxy)‐5‐β‐cholan‐24‐oic acid.