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Pharmaceutics
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Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications
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Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications

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

Deadline for manuscript submissions: closed (10 November 2021) | Viewed by 39110

Special Issue Editors

Dr. Laura Cerchia

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Guest Editor
Institute of Experimental Endocrinology and Oncology "G. Salvatore" (IEOS), National Research Council (CNR), Naples, Italy
Interests: cell-SELEX; cancer biomarker discovery; cancer cell biology and signalling; targeted therapy; chemotherapy resistance
Special Issues, Collections and Topics in MDPI journals
Dr. Simona Camorani

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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 signalling; targeted delivery system; targeted therapy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The mainstay of a therapeutic intervention is to specifically target diseased cells or tissues at high accuracy with 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 while sparing the healthy ones. Oligonucleotide aptamers, analogously to protein antibodies, interact tightly with their targets because of their complex shapes, thus representing a useful class of molecular recognition probes in various diagnostic and therapeutic applications. The quick chemical production, design flexibility, and versatile chemical modification that allow different conjugation chemistries renders aptamers 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 a great concern, as it is their high production costs: both 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 smaller size, higher stability, cheaper cost for synthesis, minimal inter-batch variability, and lack of immunogenicity. The development of actively targeted aptamer-based therapeutics will, therefore, improve methods for the delivery of conventional drugs and innovative therapeutics and will open the possibility to access lower cost 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

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Published Papers (9 papers)

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Research

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20 pages, 5088 KiB  
Article
Selective Photo-Assisted Eradication of Triple-Negative Breast Cancer Cells through Aptamer Decoration of Doped Conjugated Polymer Nanoparticles
by Luis Exequiel Ibarra, Simona Camorani, Lisa Agnello, Emilia Pedone, Luciano Pirone, Carlos Alberto Chesta, Rodrigo Emiliano Palacios, Monica Fedele and Laura Cerchia
Pharmaceutics 2022, 14(3), 626; https://doi.org/10.3390/pharmaceutics14030626 - 12 Mar 2022
Cited by 28 | Viewed by 3959 | Correction
Abstract
Photodynamic therapy (PDT) may be an excellent alternative in the treatment of breast cancer, mainly for the most aggressive type with limited targeted therapies such as triple-negative breast cancer (TNBC). We recently generated conjugated polymer nanoparticles (CPNs) as efficient photosensitizers for the photo-eradication [...] Read more.
Photodynamic therapy (PDT) may be an excellent alternative in the treatment of breast cancer, mainly for the most aggressive type with limited targeted therapies such as triple-negative breast cancer (TNBC). We recently generated conjugated polymer nanoparticles (CPNs) as efficient photosensitizers for the photo-eradication of different cancer cells. With the aim of improving the selectivity of PDT with CPNs, the nanoparticle surface conjugation with unique 2’-Fluoropyrimidines-RNA-aptamers that act as effective recognition elements for functional surface signatures of TNBC cells was proposed and designed. A coupling reaction with carbodiimide was used to covalently bind NH2-modified aptamers with CPNs synthetized with two polystyrene-based polymer donors of COOH groups for the amide reaction. The selectivity of recognition for TNBC membrane receptors and PDT efficacy were assayed in TNBC cells and compared with non-TNBC cells by flow cytometry and cell viability assays. Furthermore, in vitro PDT efficacy was assayed in different TNBC cells with significant improvement results using CL4, sTN29 and sTN58 aptamers compared to unconjugated CPNs and SCR non-specific aptamer. In a chemoresistance TNBC cell model, sTN58 was the candidate for improving labelling and PDT efficacy with CPNs. We proposed sTN58, sTN29 and CL4 aptamers as valuable tools for selective TNBC targeting, cell internalization and therapeutic improvements for CPNs in PDT protocols. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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17 pages, 1910 KiB  
Article
Development, Characterization, and In Vivo Evaluation of a Novel Aptamer (Anti-MUC1/Y) for Breast Cancer Therapy
by Huma Khan, Vaidehi Makwana, Sofia Nascimento dos Santos, Carlos Eduardo Bonacossa de Almeida, Ralph Santos-Oliveira and Sotiris Missailidis
Pharmaceutics 2021, 13(8), 1239; https://doi.org/10.3390/pharmaceutics13081239 - 11 Aug 2021
Cited by 11 | Viewed by 2806
Abstract
MUC1, the transmembrane glycoprotein Mucin 1, is usually found to be overexpressed in a variety of epithelial cancers playing an important role in disease progression. MUC1 isoforms such as MUC1/Y, which lacks the entire variable number of tandem repeat region, are involved in [...] Read more.
MUC1, the transmembrane glycoprotein Mucin 1, is usually found to be overexpressed in a variety of epithelial cancers playing an important role in disease progression. MUC1 isoforms such as MUC1/Y, which lacks the entire variable number of tandem repeat region, are involved in oncogenic processes by enhancing tumour initiation. MUC1/Y is therefore considered a promising target for the identification and treatment of epithelial cancers; but so far, the precise role of MUC1/Y remains to be elucidated. In this work, we developed and identified a DNA aptamer that specifically recognizes the splice variant MUC1/Y for the first time. The DNA aptamer could bind to a wide variety of human cancer cells, and treatment of MUC1/Y positive cells resulted in reduced growth in vitro. Moreover, MUC1/Y aptamer inhibited the tumour growth of breast cancer cells in vivo. The present study highlights the importance of targeting MUC1/Y for cancer treatment and unravels the suitability of a DNA aptamer to act as a new therapeutic tool. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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15 pages, 4933 KiB  
Article
Targeted Therapy of Hepatocellular Carcinoma Using Gemcitabine-Incorporated GPC3 Aptamer
by Jun Young Park, Ju Ri Chae, Ye Lim Cho, Youndong Kim, Dasom Lee, Jeong Kyun Lee and Won Jun Kang
Pharmaceutics 2020, 12(10), 985; https://doi.org/10.3390/pharmaceutics12100985 - 18 Oct 2020
Cited by 9 | Viewed by 3743
Abstract
Hepatocellular carcinoma (HCC) is the most common malignancy of the liver, which can progress rapidly and has a poor prognosis. Glypican-3 (GPC3) has been proposed to be an important diagnostic biomarker and therapeutic target for HCC. Aptamers have emerged as promising drug delivery [...] Read more.
Hepatocellular carcinoma (HCC) is the most common malignancy of the liver, which can progress rapidly and has a poor prognosis. Glypican-3 (GPC3) has been proposed to be an important diagnostic biomarker and therapeutic target for HCC. Aptamers have emerged as promising drug delivery vehicles because of their high binding affinity for target molecules. Herein, we developed G12msi, a gemcitabine-incorporated DNA aptamer, targeting GPC3, and evaluated its binding specificity and anti-tumor efficacy in GPC3-overexpressing HCC cell lines and murine xenograft models. GPC3-targeted aptamers were selected by using the SELEX process and the chemotherapy drug gemcitabine was internally incorporated into the aptamer. To determine the binding affinity and internalization of the G12msi, flow cytometry and confocal microscopy were performed on GPC3-positive HepG2, Hep3B, and Huh7 cells, as well as a GPC3-negative A431 cell. The anti-tumor activities of G12msi were evaluated with in vitro and in vivo models. We found that G12msi binds to GPC3-overexpressing HCC tumor cells with high specificity and is effectively internalized. Moreover, G12msi treatment inhibited the cell proliferation of GPC3-positive HCC cell lines with minimal cytotoxicity in control A431 cells. In vivo systemic administration of G12msi significantly inhibited tumor growth of HCC HepG2 cells in xenograft models without causing toxicity. These results suggest that gemcitabine-incorporated GPC3 aptamer-based drug delivery may be a promising strategy for the treatment of HCC. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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Review

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20 pages, 1574 KiB  
Review
Profiling Cancer Cells by Cell-SELEX: Use of Aptamers for Discovery of Actionable Biomarkers and Therapeutic Applications Thereof
by Sarah Shigdar, Lisa Agnello, Monica Fedele, Simona Camorani and Laura Cerchia
Pharmaceutics 2022, 14(1), 28; https://doi.org/10.3390/pharmaceutics14010028 - 24 Dec 2021
Cited by 24 | Viewed by 4510
Abstract
The identification of tumor cell-specific surface markers is a key step towards personalized cancer medicine, allowing early assessment and accurate diagnosis, and development of efficacious targeted therapies. Despite significant efforts, currently the spectrum of cell membrane targets associated with approved treatments is still [...] Read more.
The identification of tumor cell-specific surface markers is a key step towards personalized cancer medicine, allowing early assessment and accurate diagnosis, and development of efficacious targeted therapies. Despite significant efforts, currently the spectrum of cell membrane targets associated with approved treatments is still limited, causing an inability to treat a large number of cancers. What mainly limits the number of ideal clinical biomarkers is the high complexity and heterogeneity of several human cancers and still-limited methods for molecular profiling of specific cancer types. Thanks to the simplicity, versatility and effectiveness of its application, cell-SELEX (Systematic Evolution of Ligands by Exponential Enrichment) technology is a valid complement to the present strategies for biomarkers’ discovery. We and other researchers worldwide are attempting to apply cell-SELEX to the generation of oligonucleotide aptamers as tools for both identifying new cancer biomarkers and targeting them by innovative therapeutic strategies. In this review, we discuss the potential of cell-SELEX for increasing the currently limited repertoire of actionable cancer cell-surface biomarkers and focus on the use of the selected aptamers as components of innovative conjugates and nano-formulations for cancer therapy. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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34 pages, 3798 KiB  
Review
Aptamers in Virology—A Consolidated Review of the Most Recent Advancements in Diagnosis and Therapy
by Tejabhiram Yadavalli, Ipsita Volety and Deepak Shukla
Pharmaceutics 2021, 13(10), 1646; https://doi.org/10.3390/pharmaceutics13101646 - 9 Oct 2021
Cited by 7 | Viewed by 2792
Abstract
The use of short oligonucleotide or peptide molecules as target-specific aptamers has recently garnered substantial attention in the field of the detection and treatment of viral infections. Based on their high affinity and high specificity to desired targets, their use is on the [...] Read more.
The use of short oligonucleotide or peptide molecules as target-specific aptamers has recently garnered substantial attention in the field of the detection and treatment of viral infections. Based on their high affinity and high specificity to desired targets, their use is on the rise to replace antibodies for the detection of viruses and viral antigens. Furthermore, aptamers inhibit intracellular viral transcription and translation, in addition to restricting viral entry into host cells. This has opened up a plethora of new targets for the research and development of novel vaccines against viruses. Here, we discuss the advances made in aptamer technology for viral diagnosis and therapy in the past decade. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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32 pages, 4358 KiB  
Review
Aptamer-Functionalized Natural Protein-Based Polymers as Innovative Biomaterials
by Alessandra Girotti, Sara Escalera-Anzola, Irene Alonso-Sampedro, Juan González-Valdivieso and Francisco Javier Arias
Pharmaceutics 2020, 12(11), 1115; https://doi.org/10.3390/pharmaceutics12111115 - 19 Nov 2020
Cited by 8 | Viewed by 4154
Abstract
Biomaterials science is one of the most rapidly evolving fields in biomedicine. However, although novel biomaterials have achieved well-defined goals, such as the production of devices with improved biocompatibility and mechanical properties, their development could be more ambitious. Indeed, the integration of active [...] Read more.
Biomaterials science is one of the most rapidly evolving fields in biomedicine. However, although novel biomaterials have achieved well-defined goals, such as the production of devices with improved biocompatibility and mechanical properties, their development could be more ambitious. Indeed, the integration of active targeting strategies has been shown to allow spatiotemporal control of cell–material interactions, thus leading to more specific and better-performing devices. This manuscript reviews recent advances that have led to enhanced biomaterials resulting from the use of natural structural macromolecules. In this regard, several structural macromolecules have been adapted or modified using biohybrid approaches for use in both regenerative medicine and therapeutic delivery. The integration of structural and functional features and aptamer targeting, although still incipient, has already shown its ability and wide-reaching potential. In this review, we discuss aptamer-functionalized hybrid protein-based or polymeric biomaterials derived from structural macromolecules, with a focus on bioresponsive/bioactive systems. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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21 pages, 1138 KiB  
Review
Current Advances in the Development of Diagnostic Tests Based on Aptamers in Parasitology: A Systematic Review
by Juan David Ospina-Villa, Alondra Cisneros-Sarabia, Miryan Margot Sánchez-Jiménez and Laurence A. Marchat
Pharmaceutics 2020, 12(11), 1046; https://doi.org/10.3390/pharmaceutics12111046 - 31 Oct 2020
Cited by 8 | Viewed by 3095
Abstract
Aptamers are single-stranded DNA or RNA sequences of 20–80 nucleotides that interact with different targets such as: proteins, ions, viruses, or toxins, through non-covalent interactions and their unique three-dimensional conformation. They are obtained in vitro by the systematic evolution of ligands by exponential [...] Read more.
Aptamers are single-stranded DNA or RNA sequences of 20–80 nucleotides that interact with different targets such as: proteins, ions, viruses, or toxins, through non-covalent interactions and their unique three-dimensional conformation. They are obtained in vitro by the systematic evolution of ligands by exponential enrichment (SELEX). Because of their ability of target recognition with high specificity and affinity, aptamers are usually compared to antibodies. However, they present many advantages that make them promising molecules for the development of new methods for the diagnosis and treatment of human diseases. In medical parasitology, aptamers also represent an attractive alternative for the implementation of new parasite detection methods, easy to apply in endemic regions. The aim of this study was to describe the current advances in the development of diagnostic tests based on aptamers in parasitology. For this, articles were selected following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines, with specific inclusion and exclusion criteria. The 26 resulting articles deal with the use of aptamers for the detection of six important protozoa that affect human health. This systematic review clearly demonstrates the specificity, sensitivity and selectivity of aptamers and aptasensors, that certainly will soon become standard methods in medical parasitology. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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29 pages, 1146 KiB  
Review
Therapeutic Interventions into Innate Immune Diseases by Means of Aptamers
by Farzana Yasmeen, Hana Seo, Nasir Javaid, Moon Suk Kim and Sangdun Choi
Pharmaceutics 2020, 12(10), 955; https://doi.org/10.3390/pharmaceutics12100955 - 11 Oct 2020
Cited by 7 | Viewed by 3656
Abstract
The immune system plays a crucial role in the body’s defense system against various pathogens, such as bacteria, viruses, and parasites, as well as recognizes non-self- and self-molecules. The innate immune system is composed of special receptors known as pattern recognition receptors, which [...] Read more.
The immune system plays a crucial role in the body’s defense system against various pathogens, such as bacteria, viruses, and parasites, as well as recognizes non-self- and self-molecules. The innate immune system is composed of special receptors known as pattern recognition receptors, which play a crucial role in the identification of pathogen-associated molecular patterns from diverse microorganisms. Any disequilibrium in the activation of a particular pattern recognition receptor leads to various inflammatory, autoimmune, or immunodeficiency diseases. Aptamers are short single-stranded deoxyribonucleic acid or ribonucleic acid molecules, also termed “chemical antibodies,” which have tremendous specificity and affinity for their target molecules. Their features, such as stability, low immunogenicity, ease of manufacturing, and facile screening against a target, make them preferable as therapeutics. Immune-system–targeting aptamers have a great potential as a targeted therapeutic strategy against immune diseases. This review summarizes components of the innate immune system, aptamer production, pharmacokinetic characteristics of aptamers, and aptamers related to innate-immune-system diseases. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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23 pages, 1210 KiB  
Review
Current Perspectives on Aptamers as Diagnostic Tools and Therapeutic Agents
by Prabir Kumar Kulabhusan, Babar Hussain and Meral Yüce
Pharmaceutics 2020, 12(7), 646; https://doi.org/10.3390/pharmaceutics12070646 - 9 Jul 2020
Cited by 138 | Viewed by 9072
Abstract
Aptamers are synthetic single-stranded DNA or RNA sequences selected from combinatorial oligonucleotide libraries through the well-known in vitro selection and iteration process, SELEX. The last three decades have witnessed a sudden boom in aptamer research, owing to their unique characteristics, like high specificity [...] Read more.
Aptamers are synthetic single-stranded DNA or RNA sequences selected from combinatorial oligonucleotide libraries through the well-known in vitro selection and iteration process, SELEX. The last three decades have witnessed a sudden boom in aptamer research, owing to their unique characteristics, like high specificity and binding affinity, low immunogenicity and toxicity, and ease in synthesis with negligible batch-to-batch variation. Aptamers can specifically bind to the targets ranging from small molecules to complex structures, making them suitable for a myriad of diagnostic and therapeutic applications. In analytical scenarios, aptamers are used as molecular probes instead of antibodies. They have the potential in the detection of biomarkers, microorganisms, viral agents, environmental pollutants, or pathogens. For therapeutic purposes, aptamers can be further engineered with chemical stabilization and modification techniques, thus expanding their serum half-life and shelf life. A vast number of antagonistic aptamers or aptamer-based conjugates have been discovered so far through the in vitro selection procedure. However, the aptamers face several challenges for its successful clinical translation, and only particular aptamers have reached the marketplace so far. Aptamer research is still in a growing stage, and a deeper understanding of nucleic acid chemistry, target interaction, tissue distribution, and pharmacokinetics is required. In this review, we discussed aptamers in the current diagnostics and theranostics applications, while addressing the challenges associated with them. The report also sheds light on the implementation of aptamer conjugates for diagnostic purposes and, finally, the therapeutic aptamers under clinical investigation, challenges therein, and their future directions. Full article
(This article belongs to the Special Issue Aptamer-Based Targeted Conjugates for Diagnostic and Therapeutic Applications)
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