Liposomal Formulations of a Cholesterol-Tethered Pt(IV) Prodrug with Prolonged Circulation Time in Blood and Reduced Toxicity In vivo04/15/2020
Platinum based drugs play a crucial role as anticancer agents which are currently being used in clinic. Efficacy of this anticancer drugs are restricted by several side effects and drug resistance. Different drug targeting and delivery strategies have been applied to overcome these drawbacks over years. One of them is utilizing EPR (Enhanced Permeability and Retention) effect for targeting tumor cells including nanoparticles, liposome, macromolecules, micelles etc. Current work describes a strategy for loading the liposomal formulation with newly designed Platinum (IV) pro-drug and studies related to its therapeutic efficacy. The formulation being biodegradable and biocompatible, is efficient in cytotoxicity against various cell line was tested for its stability through human plasma, toxicity in-vivo, preferred accumulation in tumor cells at a higher ratio compared to cisplatin and finally activation to cisplatin initiating DNA damage and apoptosis in cancer cells.