Gemcitabine-retinoid prodrug loaded nanoparticles display in vitro antitumor efficacy towards drug-resilient human PANC-1 pancreatic cancer cells.

ABSTRACT: The treatment of pancreatic cancer with gemcitabine is hampered by its rapid metabolism in vivo, the dense stroma around the tumor site which prevents the drug from reaching the cancerous cells and drug resistance. To address these challenges, this study describes the preparation of a retinoid prodrug of gemcitabine, GemRA (gemcitabine conjugated to retinoic acid), and its formulation into a nanoparticulate system applicable for pancreatic cancer treatment. Retinoic acid targets stellate cells which are part of the stroma and can thus augment the delivery of gemcitabine. GemRA dissolved in dimethylsulfoxide presented efficacy towards PANC-1 (human) and mT4 (mouse) pancreatic cancer cell lines but its poor solubility in aqueous solution affects its applicability. Thus, the preparation of th

SUBMITTER: Kakwere H 

PROVIDER: S-EPMC7684797 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature