Methods and reagents are provided for specifically targeting biologically
active compounds such as antiviral and antimicrobial drugs, or prodrugs
containing the biologically active compound to specific sites such as
specific organelles in phagocytic mammalian cells. The biologically active
compound or prodrug is linked to a microparticle with a linker that is
non-specifically or specifically cleaved inside a phagocytic mammalian
cell. Alternatively, the biologically active compound or prodrug is
impregnated into a porous microparticle or coated on a nonporous
microparticle, and then coated with a coating material that is
non-specifically or specifically degraded inside a phagocytic mammalian
cell. The prodrug contains the biologically active compound linked to a
polar lipid such as ceramide with a specific linker such as a peptide that
is specifically cleaved to activate the prodrug in a phagocytic mammalian
cell infected with a microorganism. A microparticle linked antimicrobial
drug or prodrug may be used for killing a microorganism infecting a
phagocytic mammalian cell in vivo or in vitro.
