Coupling of the antiviral drug ara‐AMP to lactosaminated albumin leads to specific uptake in rat and human hepatocytes
Robert W. Jansen, Johan K. Kruijt, THEO J. C. van Berkel, Dirk K. F. Meije – 1 July 1993 – We covalently coupled 9‐β‐D‐arabinofuranosyladenine 5′‐monophosphate (ara‐AMP) to the carrier molecule lactosaminated human serum albumin using a water‐soluble carbodiimide with a two‐step conjugation method (pH 4.5 and pH 7.5) instead of the commonly used single‐step conjugation at pH 7.5. This resulted in a predominantly monomeric conjugate (lac27‐HSA–ara‐AMP9). The conjugate was stable in buffer (pH 7.4) and blood plasma.