Efficacy of edelfosine lipid nanoparticles in breast cancer cells

Abstract

Breast cancer is a heterogeneous group of neoplasms predominantly originating in the terminal duct lobular units. It represents the leading cause of cancer death in women and the survival frequencies for patients at advanced stages of the disease remain low.New treatment options need to be researched to improve these rates. The anti-tumor ether lipid edelfosine (ET) is the prototype of a novel generation of promising anticancer drugs. However it presents several drawbacks for its use in cancer therapy, including gastrointestinal and hemolytic toxicity and low oral bioavailability. To overcome these obstacles, ET was encapsulated in Precirol ATO 5 lipid nanoparticles (ET-LN), and its anti-tumor potential was in vitro tested in breast cancer. The formulated ET-LN were more effective in inhibiting cell proliferation and notably decreased cell viability, showing that the cytotoxic effect of ET was considerably enhanced when ET was encapsulated.In addition, ET and ET-LN were able to promote cell cycle arrest at G1 phase.

A unique multidrug nanomedicine made of squalenoyl-gemcitabine and alkyl-lysophospholipid edelfosine

“…On the other hand, since squalenoyl prodrugs display an amphiphilic structure that allows them to selfassemble into nanocomposites, it was hypothesized that to achieve a successful multidrug approach, the additional drug should possess an amphiphilic character too. 19 We selected the amphiphilic drug edelfosine (EF), an alkyl-lysophospholipid with proven anticancer activity in several tumors [20][21][22]. Unlike Gem, exerting anticancer activity through DNA synthesis inhibition, EF acts on a completely different pharmacological target.…”

Cancer research and therapy: Where are we today?

“…of breast cancer cells. 4 Edelfosine was encapsulated in Precirol ATO ® 5 lipid nanoparticles, by the hot homogenization method followed by high shear homogenization and ultrasonication. The optimized ET-NP was effective in inhibiting the proliferation of MCF7 breast cancer cell line at an IC50 concentration of 12.9 (±2.23) µg/mL.…”

Lipid-based nanocarriers for breast cancer treatment – comprehensive review

“…Globally, the burden and incidence rates of breast cancer are enormously increasing than the other cancers. Metastatic action of the breast tumors leaves the disease condition elusive and incurable (Aznar et al, 2013). Current therapies for breast cancer include radiation therapy -chemotherapy and endocrine therapy -has enriched the therapeutic effect but toxicity and side effects associated with these therapies are obstructing the clinical utility.…”