Polymeric Nano-Micelles as Novel Cargo-Carriers for LY2157299 Liver Cancer Cells Delivery

Nemany Abdelhamid Nemany Hanafy, Alessandra Quarta, Marzia Maria Ferraro, Luciana Dini, Concetta Nobile, Maria Luisa De Giorgi, Sonia Carallo, Cinzia Citti, Antonio Gaballo, Giuseppe Cannazza, Rosaria Rinaldi, Gianluigi Giannelli, Stefano Leporatti

Research output: Contribution to journalArticlepeer-review


LY2157299 (LY), which is very small molecule bringing high cancer diffusion, is a pathway antagonist against TGFβ. LY dosage can be diluted by blood plasma, can be captured by immune system or it might be dissolved during digestion in gastrointestinal tract. The aim of our study is to optimize a "nano-elastic" carrier to avoid acidic pH of gastrointestinal tract, colon alkaline pH, and anti-immune recognition. Polygalacturonic acid (PgA) is not degradable in the gastrointestinal tract due to its insolubility at acidic pH. To avoid PgA solubility in the colon, we have designed its conjugation with Polyacrylic acid (PAA). PgA-PAA conjugation has enhanced their potential use for oral and injected dosage. Following these pre-requisites, novel polymeric nano-micelles derived from PgA-PAA conjugation and loading LY2157299 are developed and characterized. Efficacy, uptake and targeting against a hepatocellular carcinoma cell line (HLF) have also been demonstrated.

Original languageEnglish
Pages (from-to)748
Number of pages13
JournalInternational Journal of Molecular Sciences
Issue number3
Publication statusPublished - Mar 6 2018


  • Antineoplastic Agents/administration & dosage
  • Cell Line, Tumor
  • Hepatocytes/drug effects
  • Humans
  • Micelles
  • Nanoparticles/chemistry
  • Pyrazoles/administration & dosage
  • Quinolines/administration & dosage


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