Abstract

Bilirubin (BR) is among the most potent endogenous antioxidants that originates from the heme catabolic pathway. Despite being considered as a dangerous and cytotoxic waste product at high concentrations, BR has extraordinary antioxidant effects leading to the reduction of oxidative stress and inflammation which play an important role in the development and progression of cancer. The purpose of this study is to introduce PEGylated BR nanoparticles (NPs), themselves or in combination with other anti-cancer agents. BR has been shown to be effective when loaded into various nanoparticles in cancer therapy. Interestingly, BRNPs can be manipulated to create stimuli-responsive carriers providing a sustained and controlled, as well as on-demand, release of drug in response to internal or external factors such as reactive oxygen species, glutathione, light, enzymes and acidic pH. Collectively, this review suggests that BRNPs have potential as tumor microenvironment-responsive delivery systems to effectively target various cancers.

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