Improved anticancer effects of epigallocatechin gallate using RGD-containing nanostructured lipid carriers

Abstract

The global burden of cancer have encouraged oncologists to develop novel strategies for treatment. Present study was proposed to develop Arginyl-glycyl-aspartic acid (RGD)-containing nanostructured lipid carriers (NLC) as a delivery system for improving the anticancer capability of epigallocatechin gallate (EGCG) on breast cancer cell line by attaching to integrin superfamily on cancer cells. For this purpose, RGD-containing EGCG-loaded NLC were prepared by hot homogenization technique and characterized by different techniques. Then, cytotoxic and apoptotic effects of prepared nanoparticles and their uptake into cells was evaluated. As results, the nanoparticles with particle size of 85 nm, zeta potential of -21 mV, encapsulation of 83% were prepared. Cytotoxicity and apoptosis experiments demonstrated that EGCG-loaded NLC-RGD possessed greatest apoptotic activity. Furthermore, it has been shown that, EGCG-loaded NLC-RGD causes cell cycle arresting more effective than EGCG. Therefore, loading EGCG into NLC-RGD make it more effective in both targeting and accumulation into tumour cells, which results from specialized uptake mechanism by adhesion to αvβ3 integrin. The results strengthen our hope that loading EGCG into RGD-containing NLC could possibly overcome the therapeutic limitations of EGCG and make it more effective in cancer therapy.

Molecular Targets of Epigallocatechin—Gallate (EGCG): A Special Focus on Signal Transduction and Cancer

“…In several in vitro and in vivo cancer types, EGCG has been shown to act synergistically with other natural compounds (e.g., curcumin, ascorbic acid, quercetin, genestein, caffeine) [10,12] and it has also been testing in combination with currently used chemotherapeutic drugs (e.g., doxorubicin, cisplatin, sunitinib) [13,14,15,16]. Furthermore, in order to improve EGCG bioavailability and stability, novel formulations of the catechin encapsulated in nanoparticles have been developed [17,18,19,20].…”

Induction of strong immune response against a multicomponent antigen of Mycobacterium tuberculosis in BALB/c mice using PLGA and DOTAP adjuvant

“…As a part of our interest in the synthesis of nanostructures and investigation of their application in infectious disease prevention, diagnosis, and treatment , the aim of this study was to determine the potential of a novel multicomponent subunit vaccine candidate entrapped in PLGA and DOTAP to enhance immune responses against Mtb in an animal model. As a secondary aim, the results of the current study were compared with the results of our previous studies.…”

Berries polyphenols: Nano-delivery systems to improve their potential in cancer therapy

“…On the other hand, EGCG-loaded RGD-NLC significantly increased cytotoxicity (IC50 = 38.2 M), apoptosis rate (∼ 49% of cells) and cell cycle arresting in sub-G1in MDA-MB-231 cells, with more effectiveness than free EGCG. Encapsulating EGCG into RGD-NLC also resulted in more effective accumulation and targeting into tumor cells [43].…”

“…Utilization of folic acid-polyethylene glycol NPs (FA-PEG-NPs) [40] and RGD-nanostructured lipid carriers (RGD-NLC) [43] for EGCG encapsulation, also improved its anti-tumor effects on human breast cancer in vitro [40,43]. In MCF-7 cells, EGCG-loaded FA-PEG-NPs inhibited cell proliferation in dose-dependent manner with an IC50 of 66.6 ± 0.6 g/mL.…”

“…This latter nano-delivery system was also used for the co-encapsulation of the EGCG with DOX, showing that EGCG-loaded NLC-RGD increased the apoptotic effect and cell cycle arresting of DOX, due to the increased uptake by tumors and probably downregulation of P-glycoprotein (Table 2). Increasing the DOX effects may allow the use of lower concentrations of the drug which in turn would reduce the associated side effects [43]. Table 1 summarizes the studies on anticancer effect of NPs containing EGCG.…”