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Nanotechnology-Driven Drug Repurposing: A Novel Strategy for Targeted Drug Delivery...
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Nanotechnology-Driven Drug Repurposing: A Novel Strategy for Targeted Drug Delivery and Pharmacokinetic Enhancement

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

Deadline for manuscript submissions: 25 March 2027 | Viewed by 6244

Special Issue Editors

Prof. Dr. Christos Papaneophytou

E-Mail Website
Guest Editor
Department of Life Sciences, School of Life and Health Sciences, University of Nicosia, 2417 Nicosia, Cyprus
Interests: drug development; small-molecule inhibitors; miRNAs; antimicrobial compounds
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Christos Petrou

E-Mail Website
Guest Editor
Pharmacy Programme, Department of Health Sciences, University of Nicosia, CY-1700 Nicosia, Cyprus
Interests: pharmacognosy; peptide chemistry and function; medicinal chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Nanotechnology has emerged as a powerful tool in drug repurposing, offering innovative solutions for targeted drug delivery and improved pharmacokinetics. This Special Issue, Nanotechnology-Driven Drug Repurposing: A Novel Strategy for Targeted Drug Delivery and Pharmacokinetic Enhancement, explores how nanocarriers such as liposomes, nanoparticles, micelles, and exosomes can optimize the therapeutic potential of existing drugs. By leveraging nanotechnology, repurposed drugs can overcome challenges like poor bioavailability, rapid metabolism, and off-target effects, ultimately enhancing their efficacy and safety. This Special Issue welcomes original research and review articles on cutting-edge advancements in nanoformulation strategies, surface modifications for precision targeting, in vitro and in vivo studies demonstrating enhanced pharmacodynamics, and regulatory perspectives on nano-enabled drug repurposing. We particularly encourage contributions focusing on applications in oncology, infectious diseases, neurodegenerative disorders, and metabolic conditions. By bridging the gap between nanomedicine and drug repositioning, this Special Issue aims to pave the way for cost-effective and efficient therapeutic solutions for unmet clinical needs.

Prof. Dr. Christos Papaneophytou
Prof. Dr. Christos Petrou
Guest Editors

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Keywords

  • nanotechnology
  • drug repurposing
  • targeted drug delivery
  • pharmacokinetics
  • nanocarriers

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Published Papers (4 papers)

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Research

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24 pages, 3132 KB  
Article
BSA-Based Nanoparticles for Dual Loading of Pazopanib and Enzalutamide: Formulation Optimization and In Vitro Evaluation in Breast Cancer Cells
by Gizem Ruya Topal, Kubra Kilic, Meral Sarper, Ozgur Esim, Ayhan Savaser and Yalcin Ozkan
Pharmaceutics 2026, 18(4), 475; https://doi.org/10.3390/pharmaceutics18040475 - 13 Apr 2026
Viewed by 644
Abstract
Objectives: Limited intracellular exposure can reduce the in vitro activity of pazopanib (PAZ) and enzalutamide (ENZ). This study developed bovine serum albumin (BSA) particles co-encapsulating PAZ and ENZ (PE-BSA) and evaluated physicochemical properties, release kinetics, 4T1 cellular uptake, and in vitro cytotoxicity versus [...] Read more.
Objectives: Limited intracellular exposure can reduce the in vitro activity of pazopanib (PAZ) and enzalutamide (ENZ). This study developed bovine serum albumin (BSA) particles co-encapsulating PAZ and ENZ (PE-BSA) and evaluated physicochemical properties, release kinetics, 4T1 cellular uptake, and in vitro cytotoxicity versus free drugs and single-drug particles. Methods: Drug-loaded BSA particles were prepared using a crosslinking-based method. Particle size (PS), polydispersity index (PDI), zeta potential (ZP), and encapsulation efficiency (EE) were determined. In vitro release was assessed over 48 h and fitted to kinetic models. 4T1 uptake was quantified after 2 and 4 h by intracellular drug levels. Cytotoxicity was measured by MTT at 24 and 72 h (1–100 µg/mL). Moreover, cell death analyses were conducted. Stability studies at +4 °C and serum were also carried out. Results: PE-BSA was nanoscale and monodisperse (PS 128.7 ± 2.6 nm; PDI 0.026 ± 0.01) with ZP −31.65 ± 1.13 mV and high EE (PAZ 98.59 ± 1.78%; ENZ 69.79 ± 0.02%). At 24/48 h, cumulative release from PE-BSA was 11.96/12.31% for PAZ and 52.26/85.95% for ENZ. The release kinetics were best described by the Korsmeyer–Peppas model for PAZ (r2 = 0.9578) and the Higuchi model for ENZ (r2 = 0.9605), indicating diffusion-controlled release. PE-BSA increased 4T1 uptake versus free drugs (2 h: 10.02% PAZ and 21.9% ENZ; 1.77-fold and 4.15-fold), with sustained enhancement at 4 h (2.2- and 4.69-fold, respectively). After 24 h, PE-BSA induced a markedly higher apoptotic response in 4T1 cells (32.5% early apoptosis and 0.8% late apoptosis/early necrosis) compared with free-PAZ (6.6% early apoptosis) and P-BSA (7.3% early apoptosis). Particles were stable. Conclusions: PE-BSA produced BSA particles with diffusion-governed release and enhanced 4T1 internalization, supporting albumin particles as a delivery platform to increase intracellular exposure of PAZ/ENZ in vitro. Full article
(This article belongs to the Special Issue Nanotechnology-Driven Drug Repurposing: A Novel Strategy for Targeted Drug Delivery and Pharmacokinetic Enhancement)
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20 pages, 2984 KB  
Article
Engineered Fenretinide- and Tocilizumab-Releasing Janus Nanoparticles for Site-Directed Immunochemoprevention of Squamous Cell Carcinoma of the Lung
by Daren Wang, Albert Chang, Fortune Shea, Yifei He, Richard Spinney, Jonathan D. Whitsett, Joerg Lahann and Susan R. Mallery
Pharmaceutics 2025, 17(11), 1471; https://doi.org/10.3390/pharmaceutics17111471 - 14 Nov 2025
Viewed by 1108
Abstract
Background: Both clinical and research data support the contribution of IL6-mediated local immunosuppression coupled with IL6-initiated protumorigenic processes, e.g., sustained proliferation and angiogenesis in the development of many cancers, including lung cancer. By virtue of their pharmacologic advantage, controlled release, local delivery [...] Read more.
Background: Both clinical and research data support the contribution of IL6-mediated local immunosuppression coupled with IL6-initiated protumorigenic processes, e.g., sustained proliferation and angiogenesis in the development of many cancers, including lung cancer. By virtue of their pharmacologic advantage, controlled release, local delivery formulations can provide immunochemopreventive relevant agent levels at the target site with negligible systemic agent-related effects. Bioavailability is a major challenge with chemopreventive agents. Methods: Janus nanoparticles (JNPs), however, are a versatile drug delivery platform that addresses several major cancer preventive challenges including bioavailability and retention of bioactivity, with elimination of potential deleterious effects with systemic administration. Furthermore, JNPs feature two discrete compartments that enable concurrent delivery of two chemically distinct agents with complementary mechanisms of action. Results: Our data show that the synthetic vitamin A derivative, fenretinide (4HPR), and the IL6R inhibitor, tocilizumab (TCZ), inhibit pathways integral for the development of lung cancer. Initial molecular modeling and kinase activity assays confirmed that 4HPR serves as a competitive inhibitor for active-site ATP binding of two key IL6 downstream kinases (JAK1, CK2). Concurrent RNA-seq analyses that employed Qiagen Ingenuity Pathway Analysis showed significant inhibition of canonical pathways associated with DNA replication and division in conjunction with significant activation of immunogeneic cell death and TREM 1 signaling pathways and showed the immune-augmenting, cancer-preventive impact of 4HPR-TCZ treatment on gene expression in premalignant lung epithelial cells. Subsequent qRT-PCR analyses corroborated the RNA seq findings and demonstrated 3- to 6-fold increased expression of TREM 1 and immunogenic cell death genes, such as TREM1 and NLRC4 and HSPA6 and DDTT3, respectively. These data collectively guided the development of human serum albumin–chitosan JNPs for the co-delivery of 4HPR and TCZ, respectively. 4HPR-TCZ JNP characterization studies demonstrated high circularities and stability in suspension, as shown by consistency in diameter and minimal changes to the polydispersity index, while confocal microscopy confirmed their biocompartmental nature. Subsequent tertiary chemoprevention in vivo studies that employed a highly aggressive human lung cancer cell line showed that JNPs releasing 4HPR and 4HPR-TCZ significantly reduced tumor volume, as assessed by vital tumor tissue, suppressed proliferation, increased apoptosis, and promoted intratumor vascular instability. Conclusions: Collectively, these studies elucidate 4HPR-TCZ in vitro chemopreventive mechanisms of action and demonstrate proof of concept for JNP-4HPR-TCZ in vivo efficacy. Full article
(This article belongs to the Special Issue Nanotechnology-Driven Drug Repurposing: A Novel Strategy for Targeted Drug Delivery and Pharmacokinetic Enhancement)
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18 pages, 1845 KB  
Article
Comprehensive Analytical Studies on the Solubility and Dissolution Rate Enhancement of Tadalafil with Type IV Lipid Formulations
by Günay Husuzade, Burcu Demiralp, Hakan Nazlı, Tuğçe Boran and Sevgi Güngör
Pharmaceutics 2025, 17(11), 1436; https://doi.org/10.3390/pharmaceutics17111436 - 7 Nov 2025
Viewed by 2029
Abstract
Background: This work aimed to enhance the solubility of Tadalafil (TDL), a BCS Class II drug, by preparing Type IV lipid-based formulations. Methods: Type IV formulations were prepared using surfactants and/or hydrophilic co-surfactants, resulting in oil-free systems. Results: Based on [...] Read more.
Background: This work aimed to enhance the solubility of Tadalafil (TDL), a BCS Class II drug, by preparing Type IV lipid-based formulations. Methods: Type IV formulations were prepared using surfactants and/or hydrophilic co-surfactants, resulting in oil-free systems. Results: Based on the solubility test, Transcutol® HP exhibited the highest solubility for TDL (48.33 ± 0.004 mg/mL) and was selected as the co-surfactant. Among surfactants, Kolliphor® PS80 (42.74 ± 2.29 mg/mL), Kolliphor® EL (41.87 ± 2.50 mg/mL), Kollisolv® PEG 400 (40.70 ± 0.30 mg/mL), and Kolliphor® HS15 (31.40 ± 3.63 mg/mL) demonstrated high solubilization capacity. These were used to prepare formulations without the addition of an oil phase. The developed formulations resulted in a system with a nano-droplet size (<50 nm) and PDI values < 0.3, which was clear, transparent, and resistant to pH dilutions. The optimum Type IV lipid formulations were further characterized and demonstrated good thermodynamic stability under temperature and pH changes. The optimized formulation was adsorbed onto different carriers and transformed into solid TDL-loaded formulations. The in vitro dissolution rate of the drug from the solidified lipid formulations was studied in various dissolution media. It was observed that the solid formulations prepared with Neusilin US2® (2:1) exhibited a significantly higher dissolution of over 95% within 5 min compared to the marketed product. The in vitro lipolysis studies demonstrated that F2 formulation maintained TDL in a supersaturated state throughout digestion, with limited enzymatic degradation of the excipients. Cytotoxicity evaluation using the MTT assay in Caco-2 cells confirmed the biocompatibility of both drug-free and TDL-loaded formulations, with IC50 values of 19.55 µg/mL and 17.55 µg/mL, respectively. Conclusions: The overall results suggested that the developed solid Type IV lipid formulations can improve the dissolution rate of TDL, which would potentially lead to an improvement in its oral bioavailability and, consequently, a reduction in the treatment dose as a safe delivery system. Full article
(This article belongs to the Special Issue Nanotechnology-Driven Drug Repurposing: A Novel Strategy for Targeted Drug Delivery and Pharmacokinetic Enhancement)
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Review

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26 pages, 1121 KB  
Review
Strategic Objectives of Nanotechnology-Driven Repurposing in Radiopharmacy—Implications for Radiopharmaceutical Repurposing (Beyond Oncology)
by María Jimena Salgueiro and Marcela Zubillaga
Pharmaceutics 2025, 17(9), 1159; https://doi.org/10.3390/pharmaceutics17091159 - 3 Sep 2025
Cited by 2 | Viewed by 1737
Abstract
The integration of nanotechnology into drug repurposing strategies is redefining the development landscape for diagnostic, therapeutic, and theranostic agents. In radiopharmacy, nanoplatforms are increasingly being explored to enhance or extend the use of existing radiopharmaceuticals, complementing earlier applications in other biomedical fields. Many [...] Read more.
The integration of nanotechnology into drug repurposing strategies is redefining the development landscape for diagnostic, therapeutic, and theranostic agents. In radiopharmacy, nanoplatforms are increasingly being explored to enhance or extend the use of existing radiopharmaceuticals, complementing earlier applications in other biomedical fields. Many of these nanoplatforms evolve into multifunctional systems by incorporating additional imaging modalities (e.g., MRI, fluorescence) or non-radioactive therapies (e.g., photodynamic therapy, chemotherapy). These hybrid constructs often emerge from the reformulation, repositioning, or revival of previously approved or abandoned compounds, generating entities with novel pharmacological, pharmacokinetic, and biodistribution profiles. However, their translational potential faces significant regulatory hurdles. Existing frameworks—typically designed for single-modality drugs or devices—struggle to accommodate the combined complexity of nanoengineering, radioactive components, and integrated functionalities. This review examines how these systems challenge current norms in classification, safety assessment, preclinical modeling, and regulatory coordination. It also addresses emerging concerns around digital adjuncts such as AI-assisted dosimetry and software-based therapy planning. Finally, the article outlines international initiatives aimed at closing regulatory gaps and provides future directions for building harmonized, risk-adapted frameworks that support innovation while ensuring safety and efficacy. Full article
(This article belongs to the Special Issue Nanotechnology-Driven Drug Repurposing: A Novel Strategy for Targeted Drug Delivery and Pharmacokinetic Enhancement)
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