Targeted delivery of therapeutic and diagnostic agents to cancer sites has significant potential
to improve the therapeutic outcome of treatment while minimizing severe side effects. It is widely
accepted that decoration of the drug delivery systems with targeting ligands that bind specifically to the
receptors on the cancer cells is a promising strategy that may substantially enhance accumulation of
anticancer agents in the tumors. Due to the transformed cellular nature, cancer cells exhibit a variety of
overexpressed cell surface receptors for peptides, hormones, and essential nutrients, providing a
significant number of target candidates for selective drug delivery. Among others, luteinizing hormonereleasing
hormone (LHRH) receptors are overexpressed in the majority of cancers, while their
expression in healthy tissues, apart from pituitary cells, is limited. The recent studies indicate that
LHRH peptides can be employed to efficiently guide anticancer and imaging agents directly to
cancerous cells, thereby increasing the amount of these substances in tumor tissue and preventing
normal cells from unnecessary exposure. This manuscript provides an overview of the targeted drug
delivery platforms that take advantage of the LHRH receptors overexpression by cancer cells.
Keywords: Cancer, drug delivery systems, GnRH, LHRH, nanoparticles, targeted delivery.
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