Biotin in the targeted transport of drugs and nanoparticles
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Keywords

biotin, selective drug delivery systems, anticancer targeted therapy, types of intracellular transport, cellu-lar in vitro models for studies of biotinylated nanoparticles

Abstract

Biotin is an essential component needed for eukaryotic cell proliferation. Its intracellular functions include mainly histone biotinylation and it is a carboxylase cofactor. Biotin requires specific transporters in cell membranes to enable its internalization due to its hydrophilicity. For many years, it has been postulated that the Sodium Dependent Multivitamin Transporter (SMVT) fulfills this role. The SMVT protein gene (SLC5A6) is expressed in mammalian cells as three isoforms - 50, 68, and 140 kDa, respectively. Its overexpression has been confirmed in few types of cancer cells. Therefore biotin is considered as a ligand selectively directing the transport of anticancer substances. However, there are some reports showing that other monocarboxylate transporters (MCTs) can participate in the uptake of this vitamin. The pathways of transport mechanism responsible for the internalization of biotinylated drug delivery systems, or even biotin itself are unknown. Considered transport pathways primarily include endocytosis: phagocytosis, macropinocytosis, clathrin-mediated endocytosis, caveolin-mediated endocytosis, and others. Biotinylated drug delivery systems, such as polystyrene nanoparticles, liposomes, and PAMAM dendrimers exhibit selective accumulation in certain cancer tissues, offering hope for their potential use in targeted therapy. However, the lack of a comprehensive understanding of the fundamental transport processes of biotinylated drug delivery systems poses a significant barrier to obtain promising practical clinical applications. The aim of this work is to systematize these issues by attempting to clearly determine whether SMVT is only transporter or also a receptor of endocytosis, essential for the internalization of biotinylated active agents and nanoparticles

https://doi.org/10.7862/rc.2026.3
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