Abstract
Active targeting is a valuable and promising approach with which to enhance the therapeutic efficacy of nanodelivery systems, and the development of tumor-targeted nanoparticles has therefore attracted much research attention. In this field, the research carried out in Italian Pharmaceutical Technology academic groups has been focused on the development of actively targeted nanosystems using a multidisciplinary approach. To highlight these efforts, this review reports a thorough description of the last 10 years of Italian research results on the development of actively targeted nanoparticles to direct drugs towards different receptors that are overexpressed on cancer cells or in the tumor microenvironment. In particular, the review discusses polymeric nanocarriers, liposomes, lipoplexes, niosomes, solid lipid nanoparticles, squalene nanoassemblies and nanobubbles. For each nanocarrier, the main ligands, conjugation strategies and target receptors are described. The literature indicates that polymeric nanoparticles and liposomes stand out as key tools for improving specific drug delivery to the site of action. In addition, solid lipid nanoparticles, squalene nanoparticles and nanobubbles have also been successfully proposed. Taken together, these strategies all offer many platforms for the design of nanocarriers that are suitable for future clinical translation.
Highlights
Cancer is a leading cause of death worldwide and has a significant impact on society in terms of productivity loss and poor health-related quality of life
Both in vitro and in vivo, it has been shown that nanocarriers that are intended for active targeting achieve the selectivity of uptake by tumor cells through endocytosis and/or receptor-mediated cytotoxicity of traditional drugs or other active compounds such as nucleic acids and products of plant origin [18]
Far from being an exhaustive list of the different ligand-receptor strategies that have been exploited by Italian researchers and that will be described in this review, this chapter is intended to emphasize the fact that the search for good anticancer targets and targeting ligands continues and is strongly stimulated by the heterogeneous and adaptive nature of many tumor types
Summary
Cancer is a leading cause of death worldwide and has a significant impact on society in terms of productivity loss and poor health-related quality of life. It should be noted that the performance of targeted anticancer nanomedicine significantly depends on the properties of the vehicles (size, surface charge, stability, degradability, safety, etc.), the ligands (nature, chemical binding, density, availability, etc.), the therapeutic agents (type, target, loading and efficiency, release, etc.) and other indications (tumor category, volume, stage, receptor density, heterogeneity, accessibility, etc.), with all of the factors intimately interacting with each other [2] In various studies, both in vitro and in vivo, it has been shown that nanocarriers that are intended for active targeting achieve the selectivity of uptake by tumor cells through endocytosis and/or receptor-mediated cytotoxicity of traditional drugs or other active compounds such as nucleic acids and products of plant origin [18]. NPs are not within the scope of this review, they play an important role in cancer nanomedicine
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