nanoparticle SN-38-encapsulated micelle formulation SNB-101

A nanoparticle-based formulation consisting of double core-shell (DUCS) micelles containing 7-ethyl-10-hydroxy-camptothecin (SN-38), the active, hydrophobic metabolite of the prodrug irinotecan, with potential antineoplastic activity. Upon intravenous administration, nanoparticle SN-38-encapsulated micelle formulation SNB-101 diffuses into the tumor site and the SN-38 moiety binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, which results in DNA breaks, inhibition of DNA replication, and apoptosis. Compared to SN-38 alone, this formulation increases the water solubility of the poorly soluble drug SN-38, and due to the stability of this formulation, it has a much longer circulation time and reduces toxicity to normal, healthy tissues.