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Mechanisms of Different Anticancer Drugs
Published in Anjana Pandey, Saumya Srivastava, Recent Advances in Cancer Diagnostics and Therapy, 2022
Anjana Pandey, Saumya Srivastava
Melphalan, also called as L-phenylalanine mustard, was first synthesized in 1953. Phenylalanine was a precursor for melanin synthesis; therefore, melphalan was initially used for the treatment of malignant melanoma. Its effect has been observed in other types of cancer such as ovarian cancer and multiple myeloma (Thirumaran et al., 2007). Melphalan can be administered orally as well as parenterally.
Investigation of characterization and cytotoxic effect of PEGylated nanoliposomal containing Melphalan on ovarian cancer: an in vitro study
Published in Journal of Experimental Nanoscience, 2021
Seyedeh Masoomeh Sadat Mirnezami, Amir Heydarinasab, Azim Akbarzadeh, Mehdi Arjmand
Melphalan (MEL; Alkeran®) is an alkylating agent that stops tumor growth by cross-linking guanine bases in two strands of deoxyribonucleic acid (DNA) and a direct attack on DNA. It is used to treat a variety of cancers, e.g. multiple myeloma cancer, ovarian cancer, and breast cancer [8]. In recent years, nanotechnology has been widely used to improve a variety of common treatments for cancer [9]. Nanotechnology involves the design, synthesis, and description of materials and devices organized on a nanoscale in at least one dimension, and their characteristics are used to diagnose and treat diseases [8,10]. Among nano-based drug delivery systems, nanolipids, such as liposomes, have been successfully used in clinical applications, and most of them have been approved by the Food and Drug Administration (FDA) of the USA [11]. Liposomes are phospholipid vesicles composed of a hydrophobic tail and a hydrophilic head and can encapsulate water- and lipid-soluble drugs in the liposome space and hydrophobic space, respectively [12]. The structural components of the liposome are synthetic amphiphilic or phospholipids, which combine with sterol lipids, such as cholesterol, to affect membrane permeability. Thin-film hydration is the most common preparation for liposomes, in which lipid components are dissolved in an organic solvent, which is evaporated by rotational evaporation followed by the re-watering of the film in an aqueous solvent [13]. Instability is one of the drawbacks of liposomes, as they are transferred to proteins in the blood and removed from the bloodstream by macrophages in the liver [14]. Therefore, the circulation time of liposomes in the blood increases by covering their surface with hydrophilic polymers, e.g. polyethylene glycol (PEG), which is a non-toxic and FDA approved compound [15]. PEGylated liposomes can be formulated with different molar ratios of their constituents to vary in size, composition, and charge. Ghaffari et al. synthesized cisplatin-loaded PEGylated nanoliposome using SPC80 (soybeanphospholipids with 75% phosphatidylcholine), cholesterol, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)] (DSPE‐MPEG) (85:10:5 weight ratio), and evaluated the cytotoxicity of the nanoformulation on breast cancer MCF-7 cells. The results showed that nanoformulation with a size of 119.7 ± 2.1 nm and zeta potential of −26.03 ± 1.34 mv demonstrated 1.6-fold higher toxicity compared to the standard drug (half maximal inhibitory concentration (IC50) = 34.7 and 56.5 µg/mL, respectively) [16].