A small molecule nanodrug consisting of amphiphilic targeting ligand chemotherapy drug conjugate for targeted cancer therapy.
Targeted drug delivery is a broadly applicable approach for cancer therapy. However, the nanocarrier based targeted delivery system suffers from batch to batch variation, quality concerns and carrier related toxicity issues. Thus, to develop a carrier free targeted delivery system with nanoscale characteristics is very attractive. Here, a novel targeting small molecule nanodrug self delivery system consisting of targeting ligand and chemotherapy drug was constructed, which combined the advantages of small molecules and nano assemblies together and showed excellent targeting ability and long blood circulation time with well defined structure, high drug loading ratio and on demand drug release behavior. As a proof of concept, lactose (Lac) and doxorubicin (DOX) were chosen as the targeting ligand and chemotherapy drug, respectively. Lac and DOX were conjugated through a pH responsive hydrazone group. For its intrinsic amphiphilic property, Lac DOX conjugate could self assemble into nanoparticles in water. Both in vitro and in vivo assays indicated that Lac DOX nanoparticles exhibited enhanced anticancer activity and weak side effects. This novel active targeting nanodrug delivery system shows great potential in cancer therapy.
Journal of controlled release official journal of the Controlled Release Society