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Liposomal rifamycin (specifically liposomal rifamycin SV) is a liposomal formulation of the ansamycin antibiotic rifamycin SV, being investigated for its potential repurposing as an antineoplastic agent. Developed by researchers at Northeastern University and the University of Campinas, the formulation encapsulates rifamycin SV within PEGylated liposomes composed of egg phosphatidylcholine, cholesterol, and DOPE-PEG5k. This lipid-based delivery system is designed to enhance the stability and biocompatibility of rifamycin SV, preventing its precipitation in physiological conditions and reducing its hemolytic potential. In preclinical studies, liposomal rifamycin demonstrated significant cytotoxic activity against various cancer cell lines, including breast cancer (MCF-7, MDA-MB-231), glioblastoma (U87), and lung cancer (A549), as well as in 3D tumor spheroid models. The formulation can also be functionalized with tumor-targeting antibodies, such as the nucleosome-binding monoclonal antibody 2C5, to improve cellular uptake and therapeutic efficacy.
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