Posted by A new book chapter titled “Metallocyclodextrins for Cancer Chemotherapy” by Susana Santos Braga is published in the ACS Symposium series e-book ‘Anticancer Potential of Macrocyclic Metal Complexes’, edited by Wani et al., offers insights into potential new approaches for cancer treatment.
The chapter examines the use of metallocyclodextrins as antitumoral agents, both as active drugs and as synergistic carriers for existing clinical drugs. The work focuses on three main categories of metallocyclodextrins with promising applications in cancer therapy:
1) Platinocyclodextrins: These compounds comprise aminoplatinum cyclodextrins and selenated platinum cyclodextrins. The first ones, set to combine the well-known anticancer properties of cisplatin with the solubilising capabilities of cyclodextrins, are attractive in theory, but tricky to achieve efficacy in vitro as the bulky cyclodextrin cannot penetrate cells unlike the planar and small structure of the lead drug, cisplatin. The class of selenocyclodextrins permits the platinated fragment to separate from the cyclodextrin upon contact with the cells to enter them freely and exert its activity. Notably, some compounds in this class are patented for leukaemia.
2) Cyclodextrin-appended metalloporphyrins and metallophthalocyanines: The metallic heterocycle in these compounds acts as a photosensitiser, generating reactive oxygen species when activated by light, while the cyclodextrin component enhances their solubility and potential for targeted delivery. These compounds are designed to be used in photodynamic therapy, a treatment modality that uses light activation to induce cytotoxic effects only in the irradiated tissues. The aim is to reduce the systemic side effects typically observed in traditional chemotherapy.
3) Cyclodextrin-based delivery systems: loaded with a platinum prodrug, these systems explore the complexation properties of cyclodextrins to obtain self-assembled micelles with a PLGA core and a biocompatible PEGylated surface.
Braga’s chapter provides a comprehensive overview of the current state of research in this field, discussing the structures, properties and potential applications of these metallocyclodextrin compounds. The author also explores the challenges and opportunities in translating this research into clinical applications. The publication of this chapter represents a significant step forward in understanding the potential applications of metallocyclodextrins in cancer chemotherapy, understanding what are the best new research avenues as well as the pitfalls of research that are revealed by less successful previous reports. As research in this field continues to advance, the ideas conveyed in this chapter will hopefully help researchers reflect, design and develop new treatment strategies to address the complex challenges posed by cancer.
Susana Santos Braga (2025) Metallocyclodextrins for Cancer Chemotherapy. ACS Symposium Series Vol. 1492. Anticancer Potential of Macrocyclic Metal Complexes, Chapter 7, pp 153-169
eISBN: 9780841296787. DOI: 10.1021/bk-2025-1492.ch007