Polyphenol‐Based Nanosystems for Next‐Generation Cancer Therapy: Multifunctionality, Design, and Challenges

Abstract

With the continuous updating of cancer treatment methods and the rapid development of precision medicine in recent years, there are higher demands for advanced and versatile drug delivery systems. Scientists are committed to create greener and more effective nanomedicines where the carrier is no longer limited to a single function of drug delivery. Polyphenols, which can act as both active ingredients and fundamental building blocks, are being explored as potential multifunctional carriers that are efficient and safe for design purposes. Due to their intrinsic anticancer activity, phenolic compounds have shown surprising expressiveness in ablation of tumor cells, overcoming cancer multidrug resistance (MDR), and enhancing immunotherapeutic efficacy. This review provides an overview of recent advances in the design, synthesis, and application of versatile polyphenol‐based nanosystems for cancer therapy in various modes. Moreover, the merits of polyphenols and the challenges for their clinical translation are also discussed, and it is pointed out that the novel polyphenol delivery system requires further optimization and validation.

A Critical Appraisal of the Protective Activity of Polyphenolic Antioxidants against Iatrogenic Effects of Anticancer Chemotherapeutics

“…Several studies have highlighted the correlation between the consumption of polyphenol-rich foods and a lower incidence of different types of cancer, chronic heart diseases, and neurodegenerative diseases [4][5][6]. However, only a limited number of clinical studies have proven the distinct impact of dietary polyphenols on cancer prevention [24,25].…”

“…Nanodelivery systems may have the potential to improve their therapeutic efficacy. While the reader may refer to recent, more exhaustive reviews on these topics [4,10], herein we would like to draw attention to some promising applications in CNS diseases [46] or in cancer prevention and therapy [99].…”

“…Several studies have highlighted the relationships between dietary polyphenols and lower incidences of cancer, chronic heart diseases, and neurodegenerative syndromes [4][5][6][7]. The Mediterranean diet is associated with a reduced risk of cardiovascular disease, thanks to an adequate intake of olive oil, red wine, and anthocyanin-containing fruits and vegetables [8,9].…”

Endothelin-1 and Its Role in Cancer and Potential Therapeutic Opportunities

“…Cancer therapies such as chemotherapy present various challenges, including severe side effects, resistance to chemotherapeutic drugs impacting their efficacy and impaired tumour clearance. Subsequently, continued efforts to improve techniques such as chemotherapy are ongoing [ 48 ]. One such effort is to supplement chemotherapy with polyphenols as anti-tumour agents.…”

“…Polyphenols are phytochemicals with complex structures composed of catechol and gallol groups, possessing multiple hydroxyls, giving rise to their potent antioxidant properties. Their structures allow the formation of many different interactions, allowing them to bind to various substrates [ 48 ].…”