Abstract
Soluble copolymers of -(2-hydroxypropyl)methacrylamide (HPMA) were prepared containing either oligopeptide side chains terminating in p-nitroaniline, or oligopeptide sequences forming crosslinks between polymer chains. Such copolymers have potential as targetable drug carriers and already it has been shown that oligopeptide side chains and oligopeptide crosslinks are degraded intracellularly by lysosomal enzymes. The susceptibility of these oligopeptide sequences to degradation on incubation with rat plasma or rat serum was evaluated by monitoring either the liberation of p-nitroaniline or, with the crosslinked polymers, the change in molecular weight distribution. Release of p-nitroaniline from some of the polymers was not detectable, and from others proceeded very slowly, the maximum rate being from the side chain Gly-Gly-Phe-Leu-Glv-Phe-NAp where 5.1% of the bound p-nitroaniline was released by rat serum over a 5 h incubation period. No cleavage of crosslinked HPMA copolymers by plasma or serum was detectable even after a 24 h incubation period.
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