Abstract
Simple SummaryOne of the primary causes of chemotherapy failure is the occurrence of cancer multidrug resistance (MDR). Uncontrolled growth of resistant tumor cells leads to metastasis and recurrence, associated with high mortalities. Ferrocifens have been shown to possess anticancer properties via an original mechanism dependent on redox properties and generation of active metabolites that can cause disruption of cell metabolism. However, these molecules are highly insoluble in water, requiring a formulation stage before being administered in vivo. Lipid nanocapsules (LNCs) have already demonstrated their ability to successfully encapsulate various hydrophobic therapeutic agents, such as ferrocifens, and offer the option of surface modification, making it possible to adapt the pharmacological behavior of the nanocarrier. The aim of this review is to give, for the first time, an overview of the in vitro and in vivo studies performed with ferrocifen-loaded LNCs on several MDR cancers.Resistance of cancer cells to current chemotherapeutic drugs has obliged the scientific community to seek innovative compounds. Ferrocifens, lipophilic organometallic compounds composed of a tamoxifen scaffold covalently bound to a ferrocene moiety, have shown very interesting antiproliferative, cytotoxic and immunologic effects. The formation of ferrocenyl quinone methide plays a crucial role in the multifaceted activity of ferrocifens. Lipid nanocapsules (LNCs), meanwhile, are nanoparticles obtained by a free organic solvent process. LNCs consist of an oily core surrounded by amphiphilic surfactants and are perfectly adapted to encapsulate these hydrophobic compounds. The different in vitro and in vivo experiments performed with this ferrocifen-loaded nanocarrier have revealed promising results in several multidrug-resistant cancer cell lines such as glioblastoma, breast cancer and metastatic melanoma, alone or in combination with other therapies. This review provides an exhaustive summary of the use of ferrocifen-loaded LNCs as a promising nanomedicine, outlining the ferrocifen mechanisms of action on cancer cells, the nanocarrier formulation process and the in vivo results obtained over the last two decades.
Highlights
The tumor volume was reduced by 40% with stealth DP1-lipid nanocapsules (LNCs) and 9% with stealth P5-LNCs compared to the untreated group and a difference of around 13% was observed between stealth DP1-LNCs and DTIC treatments
Ferrocifens are molecules endowed with multiple biological properties, including anticancer activity, that induce inhibition of cancer cell growth through apoptosis and/or senescence according to the conditions previously described
By taking advantage of the microenvironment of the tumor, these organometallic compounds might overcome the resistance of MDR cancer to apoptosis
Summary
The potential efficacy of these innovative compounds is conferred by the chemical reactivity of the organometallic complex, different from that of the metal or the organic ligands alone Amongst these complexes, the ferrocifen family consists of a ferrocene moiety covalently bound to a tamoxifen skeleton that has shown promising in vitro results against MDR cancer cell lines [11,12,13]. Since the beginning of the 21st century, these innovative NPs have received the most attention, with this surface modification aiming to improve the biodistribution and limit the side effects of the drugs [21,22,23] Within this array of nanocarriers, Heurtault et al patented a hybrid structure between polymer. The specificities of LNCs will be described, especially through their potential as ferrocifen nanocarriers, and the in vivo experiments on MDR cancers such as glioblastoma, metastatic melanoma and breast cancer will be reviewed
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