The concepts of polymer–peptide
conjugation and self-assembly
were applied to antimicrobial peptides (AMPs) in the development of
a targeted antimalaria drug delivery construct. This study describes
the synthesis of α-acetal, ω-xanthate heterotelechelic
poly(N-vinylpyrrolidone) (PVP) via reversible addition–fragmentation
chain transfer (RAFT)-mediated polymerization, followed by postpolymerization
deprotection to yield α-aldehyde, ω-thiol heterotelechelic
PVP. A specific targeting peptide, GSRSKGT, for Plasmodium
falciparum-infected erythrocytes was used to sparsely
decorate the α-chain ends via reductive amination while cyclic
decapeptides from the tyrocidine group were conjugated to the ω-chain
end via thiol–ene Michael addition. The resultant constructs
were self-assembled into micellar nanoaggregates whose sizes and morphologies
were determined by dynamic light scattering (DLS) and transmission
electron microscopy (TEM). The in vitro activity and selectivity of
the conjugates were evaluated against intraerythrocytic P. falciparum parasites.
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