This invention discloses compositions of
chloroquine-coupled active agents such as therapeutic antibodies or
insulin, including methods for their preparation. The prior art has shown that chloroquines given as
free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the
cytoplasm. The purpose of these compositions is to provide a controlled amount of
chloroquine at the same site where the
drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a
chloroquine substance coupled to a
drug directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for
therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing the
drug for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and
antibody or
insulin to their
site of action.