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.
Ferrocifens Used (Names) | Pathology | LNC Formulation | Encapsulation Efficiency (Drug Loading) | In Vivo Studies |
---|---|---|---|---|
P5 (FcdiOH) |
Glioblastoma (9L glioma cells) | Conventional LNCs | >98% (1.0 mg/g or 6.5 mg/g) | Single intratumoral injection (400 µL); ectopic model [39] |
Glioblastoma (9L glioma cells) | Conventional LNCs | 96% (1.0 mg/g or 6.5 mg/g) | Single intracranial injection by CED (60 µL, 0.36 mg/rat) + 3 irradiations of 6 Gy doses; orthotopic model [58] | |
Glioblastoma (9L glioma cells) | NFL-TBS-63 peptide-coated LNCs | (6.1 mg/mL) | Intracarotid injection (400 µL, 2.5 mg/rat); orthotopic model [28] | |
(5.5 mg/mL) | Injection by CED (60 µL, 0.36 mg/kg rat); orthotopic model [28] | |||
Glioblastoma (9L glioma cells) | Stealth LNCs | >98% (6.5 mg/g) | Single intravenous injection (400 µL, 2.4 mg/rat); ectopic model [88] | |
Single intravenous injection (400 µL, 2.4 mg/rat); orthotopic model [88] | ||||
Glioblastoma (9L glioma cells) | Stealth LNCs and conventional LNCs | (6.5 mg/g) | Intracarotid injection (400 µL, 2.4 mg/rat), orthotopic model [97] | |
CED injection (60 µL, 0.36 mg/rat), orthotopic model [97] | ||||
Glioblastoma (U87MG cells) | LNC-loaded MIAMI cells | (2.6 mg/mL) | Intratumoral injection (100 µL), heterotopic model [98] | |
Glioblastoma (U87MG cells) | LNC-loaded MIAMI cells | (6.0 mg/g of LNCs) 20 pg of P5/MIAMI cells |
Intratumoral injection (3.6 µg/mouse), orthotopic model [57] | |
Melanoma (SK-Mel28 human cells) | Stealth LNCs | 92% (6.0 mg/mL) | Repeated intravenous injection (45 mg/kg); ectopic model [59] | |
P15 (FcOHTam) |
Breast cancer (MDA-MB-231 cells) | Stealth LNCs | 100% (8.0 mg/mL) | Repeated intraperitoneal injection (2×) (20 mg/kg); ectopic model [55] |
DP1 (Ansa-FcdiOH) |
Melanoma (SK-Mel28 human cells) | Stealth LNCs | 96% (6.0 mg/mL) | Repeated intravenous injection (45 mg/kg); ectopic model [59] |
Stealth LNCs with Bcl-2 siRNA | 85% (6.0 mg/mL) | Repeated intravenous injection (45 mg/kg); ectopic model [59] | ||
Glioblastoma (9L glioma cells) | Stealth LNCs | (6.4 mg/g) | Repeated intravenous injection (10×) (20 mg/kg); ectopic model [99] | |
P53 (FctriOH) |
Glioblastoma (U87MG cells) | NFL-TBS40-63 peptide-coated LNCs | >99% (2.67 mg/g) | Intravenous injection (2×) (70 µL, 20 mg/kg); ectopic model [95] |
P722 |
Melanoma (B16F10 cells) | Stealth LNCs | 65% | Intraperitoneal injection (7 mg/kg); orthotopic model [96] |
This entry is adapted from the peer-reviewed paper 10.3390/cancers13102291