Combination of Small Molecule Prodrug and Nanodrug Delivery: Amphiphilic Drug–Drug Conjugate for Cancer Therapy

All drugs for cancer therapy face several transportation barriers on their tortuous journey to the action sites. To overcome these barriers, an effective drug delivery system for cancer therapy is imperative. Here, we develop a drug self-delivery system for cancer therapy, in which anticancer drugs can be delivered by themselves without any carriers. To demonstrate this unique approach, an amphiphilic drug-drug conjugate (ADDC) has been synthesized from the hydrophilic anticancer drug irinotecan (Ir) and the hydrophobic anticancer drug chlorambucil (Cb) via a hydrolyzable ester linkage. The amphiphilic Ir-Cb conjugate self-assembles into nanoparticles in water and exhibits longer blood retention half-life…

• NN
  National Natural Science Foundation of China

  Awards: 91127047, 21025417
• MO
  Ministry of Science and Technology of the People's Republic of China

  Awards: 2011CB933101, 2012CB821500, 2013CB834506