Newly acylated SN-38 homodimers: carrier-free nano-prodrugs for chemotherapy

Homodimers based on 7-ethyl-10-hydroxycamptothecin (SN-38) containing S₂[(CH₂)₂OC(O)]₂ bridge and acyl substituents were synthesized and used for fabrication of nano-prodrugs. The latter demonstrated remarkable dispersion and stability over one month when stored at a temperature of 4 °C, with an ideal size of nanoparticles in the range of 80–130 nm that is required for EPR effect. The homodimer containing cyclopropylacetyl substituent chain exhibited significant anticancer efficacy against the HCT-116 and A-549 cell lines, with IC50 values having been 0.07 ± 0.01 and 0.29 ± 0.02 μm, respectively.