Abstract
Triple-negative breast cancer (TNBC) is a highly aggressive type of cancer with limited therapeutic options. However, this type of cancer cells has shown overexpression of folate receptors, which bind with folic acid (FA) with high affinity. This feature can be used for targeting of nanocarriers, such as liposomes. In order to further examine the potential of increased efficacy by targeting the folate receptor, we prepared folate conjugated liposomes (DSPC/Chol/PEG/DSPE-PEG-FA) and loaded them with doxorubicin (DOX), an anticancer drug. For this, we first synthesized and verified the conjugate between FA and PEG-lipid (FA-PEG-lipid). After that, liposomes were prepared with thin film hydration method followed by probe sonication. Three different types of targeted liposomes having different concentrations of FA-PEG-lipid in their membranes (0.1 mol%, 0.5 mol%, and 1 mol%) were evaluated for their cytotoxicity (DOX-loaded liposomes) on MDA-MB-231 (epithelial human breast cancer cells), 4T1 (murine mammary carcinoma cells), and MCF7 (Human breast cancer cells); the two first are TNBC cells and overexpress FA receptor, the third does not. Cytotoxicity results proved that increasing amounts of FA on the surface of liposomes results in enhanced antitumor activity of liposomal-DOX in the case of the cancer cells, which overexpress the FA receptor.
Highlights
Published: 1 December 2020Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.Licensee MDPI, Basel, Switzerland
Even systemic chemotherapy with clinically approved drugs reflects poor response and high toxicity and develops multidrug resistance. This type of cancer cells has shown overexpression of folate receptors, which bind with folic acid (FA) with high affinity
All liposome dispersions were characterized for their size distribution and their zeta-potential (Table 1)
Summary
Published: 1 December 2020Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.Licensee MDPI, Basel, Switzerland. Triple-negative breast cancer (TNBC) owes 15–20% of all the invasive subtypes of breast cancer [3] and is characterized by absence of expression of estrogen receptors (ER), progesterone receptors (PR), and human epidermal growth factor receptor 2 (HER-2) on tumors cell membrane. This feature eliminates the benefits of endocrine therapy and treatment, mainly relies on chemotherapy [4]. Even systemic chemotherapy with clinically approved drugs reflects poor response and high toxicity and develops multidrug resistance This type of cancer cells has shown overexpression of folate receptors, which bind with folic acid (FA) with high affinity. Liposomes conjugated to the folate ligand via a polyethylene glycol (PEG) spacer have been used to deliver chemotherapeutic agents, oligonucleotides, and markers to FR-bearing tumor cells
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