Publication date: Available online 12 May 2017
Source:Advanced Drug Delivery Reviews
Author(s): Ayelet David
Since their initial discovery more than 30 years ago, tumor-homing peptides have become an increasingly useful tool for targeted delivery of therapeutic and diagnostic agents into tumors. Today, it is well accepted that cells at tumor microenvironment (TME) contributes in many ways to cancer development and progression. Tumor-homing peptide are highly suitable ligands to actively target cells at the TME owing to their small size, low immunogenicity, stability, easy manufacturing and low cost. When conjugated to nanosized medicines (nanomedicines) these ligands can interact specifically with surface receptors expressed on cells in the heterogeneous TME, improve cellular uptake of nanomedicines by target cells, and potentially impair tumor growth and progression. Moreover, peptide-modified nanomedicines can accumulate in the target tissue at higher concentrations than would small conjugates, thus increase overall target tissue exposure to the therapeutic agent, enhance therapeutic efficacy and reduce side effects. This review describes the most studied peptide–directed nanomedicines aimed at targeting cells in the TME, discusses major obstacles and principles in the design of ligands for drug targeting and provides an overview of homing peptides in ligand-targeted nanomedicines that are currently in development for cancer therapy and diagnosis.
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