Abstract

A lot of solid tumors are characterized by uncontrolled signal transduction triggered by receptors related to cellular growth. The targeting of these cell receptors with antitumor drugs is essential to improve chemotherapy efficacy. This can be achieved by conjugation of an active targeting agent to the polymer portion of a colloidal drug delivery system loaded with an antitumor drug. The goal of this minireview is to report and discuss some recent results in epidermal growth factor receptor targeting by the GE11 peptide combined with colloidal drug delivery systems as smart carriers for antitumor drugs. The minireview chapters will focus on explaining and discussing: (i) Epidermal growth factor receptor (EGFR) structures and functions; (ii) GE11 structure and biologic activity; (iii) examples of GE11 conjugation and GE11-conjugated drug delivery systems. The rationale is to contribute in gathering information on the topic of active targeting to tumors. A case study is introduced, involving research on tumor cell targeting by the GE11 peptide combined with polymer nanoparticles.

Highlights

  • Drug targeting relevance is increasing as long as the knowledge about cellular targets and precise targeting agents increases

  • GE11 is studied as a peptide ligand, selectively recognizing Epidermal growth factor receptor (EGFR) for diagnostic and therapeutic purposes with respect to EGFR-overexpressing cancer cells

  • Different types of drug delivery systems (DDS) and GE11 conjugates are proposed in the literature

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Summary

Introduction

Drug targeting relevance is increasing as long as the knowledge about cellular targets and precise targeting agents increases. Nanoparticles (NPs) made of biodegradable and biocompatible polymers present several advantages as carriers for therapeutics, such as the ability to encapsulate a wide variety of agents, including peptides, proteins, and genes, and to control drug release rates. The latter property is important when administering chemotherapeutics, because a strict control of drug release and target release can be beneficial in reducing drug toxicity and improving drug efficacy. Third-generation DDS combine the typical features of first-generation DDS (size and stability) and second-generation DDS (active targeting) with functional modules They allow for displaying complex operations through consequent logical events such as: transport through biological barriers, disposition in the target tissue, selective cell recognition, cell uptake, masking–demasking events, and controlled drug release. DDS, this minireview will focus on a specific topic, that is, the active targeting to tumors achieved by GE11 peptide combined with nanoparticulate DDS

EGFR and EGFR Targeting
Epidermal
GE11 Structure and Biologic Activity
Results in the literature confirm
Conclusions
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