Synthesis and evaluation of nanoliposomes containing epigallocatechin gallate: Experimental/ Computational Studies

Tohidlou, Mohammad; Sadeghi-Mohammadi, Sanam; Ghorbani, Mohammad; Vaezi, Zahra; Farasat, Alireza; Taghdir, Majid; Naderi-Manesh, Hossein

Synthesis and evaluation of nanoliposomes containing epigallocatechin gallate: Experimental/ Computational Studies

Document Type : Original Research

Authors

Mohammad Tohidlou ¹

Sanam Sadeghi-Mohammadi ²

Mohammad Ghorbani ¹

Zahra Vaezi ³

Alireza Farasat ⁴

Majid Taghdir ¹

Hossein Naderi-Manesh ¹

¹ Biophysics Department, Biological Sciences Faculty, Tarbiat Modares University, Tehran, Iran.

² Tuberculosis and Lung Disease Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

³ Bioactive compounds Department, Interdisciplinary Science and Technologies Faculty, Tarbiat Modares University, Tehran, Iran.

⁴ Monoclonal Antibody Research Center, Avicenna Research Institute, ACECR, Tehran, Iran.

Abstract

Matrix metalloproteinases (MMPs) are a zinc endopeptidase family that increases the metastatic behavior of human malignant tumors. Epigallocatechin gallate (EGCG) is a major component of green tea polyphenols and is used as an MMP inhibitor in cancer treatment. This study aims to develop and optimize the loading of EGCG in the liposomal delivery system in an experimental/ computational way. In this study, nanoliposomes were prepared by passive loading and thin-film hydration method. Size, zeta potential, stability, encapsulation efficiency, and nanoliposome drug release profile were investigated. Cytotoxicity of nanoliposomes was evaluated on three breast cancer cell lines using an MTT viability assay. To investigate the EGCG-Liposome interaction, coarse-grained Molecular Dynamic simulations were carried out. The mean diameter of liposome was 73.6±6.9 nm, the surface charge was -14.6 mV and the encapsulation efficiency was 78.5±7.3%. The encapsulation of EGCG into the liposome caused a continuous release of the drug after 72 h, which also increased the potency of the drug. Due to the EGCG hydrophobic properties, the major distribution is located at the hydrophobic part of the membrane. The energy and radial distribution function results indicate the stability of liposomes. Simulation results demonstrate that the majority of the drug is surrounded by liposomes, which indicates high encapsulation efficiency and confirms the developed synthesis method. Due to the low solubility of the drug, it seems that the use of liposomal carriers to deliver and release EGCG is a suitable solution to increase the efficiency of the drug.

Keywords

Epigallocatechin Gallate

Liposome

Breast Cancer

Molecular dynamics simulation

Martini Force Field

Subjects

Nanotechnology

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