Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications Volume II

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 2809

Special Issue Editors


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Guest Editor
Institute of Experimental Endocrinology and Oncology "G. Salvatore" (IEOS), National Research Council (CNR), Naples, Italy
Interests: aptamers; cell-SELEX technology; cancer-cell biology and signaling; targeted delivery system; targeted therapy
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Special Issue Information

Dear Colleagues,

The mainstay of a therapeutic intervention is to specifically target diseased cells or tissues at a high accuracy and with a low frequency of adverse side effects. One possibility to reach this goal is to use disease-specific ligands as delivery agents to drive therapeutic cargos to the diseased sites, without compromising the healthy ones. Oligonucleotide aptamers, analogous to protein antibodies, closely interact with their targets as a result of their complex shapes, thus representing a useful class of molecular recognition probes in various diagnostic and therapeutic applications. The rapid chemical production, design flexibility, and versatile chemical modification that allow different conjugation chemistries, renders aptamers as ideal targeting moieties in advanced targeted delivery strategies. Antibody-based targeted therapeutics provide high target specificity and affinity. However, their potential for immunogenicity is of great concern, as this is the reason for their high production cost; these problems may therefore limit their clinical applicability. Conversely, active disease targeting by aptamers, while preserving affinity and specificity similar to monoclonal antibodies, presents several advantages over them, including a smaller size, higher stability, cheaper cost for synthesis, minimal inter-batch variability, and lack of immunogenicity. The development of actively targeted aptamer-based therapeutics, therefore, improves methods for the delivery of conventional drugs and innovative therapeutics, and opens the possibility to access lower costs and highly effective therapies. The present Special Issue will include original research articles and review articles aimed at covering new synthetic methodologies of aptamer conjugates as well as their novel applications.

Dr. Laura Cerchia
Dr. Simona Camorani
Guest Editors

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Keywords

  • aptamer-targeted nanosystems
  • aptamer–drug conjugates
  • bifunctional aptamers
  • aptamer–antibody
  • aptamer–enzyme
  • targeted therapy
  • targeted imaging
  • targeted delivery systems

Published Papers (1 paper)

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Research

16 pages, 2598 KiB  
Article
Aptamer-Functionalized Nanoparticles Mediate PD-L1 siRNA Delivery for Effective Gene Silencing in Triple-Negative Breast Cancer Cells
by Simona Camorani, Silvia Tortorella, Lisa Agnello, Chiara Spanu, Annachiara d’Argenio, Roberto Nilo, Antonella Zannetti, Erica Locatelli, Monica Fedele, Mauro Comes Franchini and Laura Cerchia
Pharmaceutics 2022, 14(10), 2225; https://doi.org/10.3390/pharmaceutics14102225 - 18 Oct 2022
Cited by 15 | Viewed by 2544
Abstract
Small interfering RNA (siRNA) therapies require effective delivery vehicles capable of carrying the siRNA cargo into target cells. To achieve tumor-targeting, a drug delivery system would have to incorporate ligands that specifically bind to receptors expressed on cancer cells to function as portals [...] Read more.
Small interfering RNA (siRNA) therapies require effective delivery vehicles capable of carrying the siRNA cargo into target cells. To achieve tumor-targeting, a drug delivery system would have to incorporate ligands that specifically bind to receptors expressed on cancer cells to function as portals via receptor-mediated endocytosis. Cell-targeting and internalizing aptamers are the most suitable ligands for functionalization of drug-loaded nanocarriers. Here, we designed a novel aptamer-based platform for the active delivery of siRNA targeting programmed cell death-ligand 1 (PD-L1) to triple-negative breast cancer (TNBC) cells. The generated nanovectors consist of PLGA-based polymeric nanoparticles, which were loaded with PD-L1 siRNA and conjugated on their surface with a new RNA aptamer, specific for TNBC and resistant to nucleases. In vitro results demonstrated that these aptamer-conjugated nanoparticles promote siRNA uptake specifically into TNBC MDA-MB-231 and BT-549 target cells, along with its endosomal release, without recognizing non-TNBC BT-474 breast cancer cells. Their efficiency resulted in an almost complete suppression of PD-L1 expression as early as 90 min of cell treatment. This research provides a rational strategy for optimizing siRNA delivery systems for TNBC treatments. Full article
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