Innovative Boron-Based Drug Delivery Systems

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

Deadline for manuscript submissions: 31 August 2026 | Viewed by 532

Special Issue Editors


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Guest Editor
Organization for Interdisciplinary Education and Research, Neutron Therapy Research Center, Okayama University, Okayama, Japan
Interests: boron neutron capture therapy (BNCT); drug delivery systems; formulation approaches

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Guest Editor
Graduate School of Medicine, Density and Pharmaceutical Sciences, Okayama University, Okayama, Japan
Interests: peptide; boron cluster; supermolecule

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Guest Editor
Department of Neurosurgery, University of Tsukuba, Tsukuba, Japan
Interests: boron neutron capture therapy (BNCT); drug delivery systems; nanoparticles; radiobiology; medical IT; AI-based systems
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Special Issue Information

Dear Colleagues,

Boron-containing agents are central to boron neutron capture therapy (BNCT), where selective delivery of sufficient boron to tumors is a key determinant of therapeutic success. At the same time, boron-based drugs and boron-containing nanomaterials are increasingly used in other therapeutic areas, including oncology, dermatology, infectious diseases, and advanced imaging. Across these diverse applications, a rational drug delivery system (DDS) design is essential to control solubility, stability, pharmacokinetics, tissue targeting, and safety.

This Special Issue aims to highlight cutting-edge advances in boron-based drug delivery, with BNCT as a core focus while also welcoming broader work on boron-containing drugs and boron-based nanomedicine, in line with the scope of Pharmaceutics. We invite studies that address the design, formulation, and in vitro/in vivo evaluation of boron agents, as well as translational research that bridges pharmaceutical technology with clinical or preclinical applications.

For this Special Issue, submissions of original research articles and reviews are welcome. Research areas may include (but are not limited to) the following: (i) novel boron carriers for BNCT (small molecules, peptides, polymers, liposomes, nanoparticles, and hybrid systems); (ii) delivery optimization of approved or emerging boron drugs (e.g., benzoxaboroles and boronic acid–based therapeutics); (iii) formulation approaches advanced DDS platforms; (iv) boron-based nanomaterials for drug delivery and imaging; and (v) imaging, biodistribution analysis, dosimetry, and combination therapies integrating boron-based strategies with radiotherapy, chemotherapy, or immunotherapy.

We look forward to receiving your contributions.

Dr. Makoto Shirakawa
Dr. Tomohiro Tanaka
Dr. Alexander Zaboronok
Guest Editors

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Keywords

  • boron neutron capture therapy (BNCT)
  • boron-containing drug delivery
  • boron-based nanomedicine
  • benzoxaborole and boronic acid drugs
  • targeted cancer therapy
  • imaging and dosimetry

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Published Papers (1 paper)

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13 pages, 1577 KB  
Article
Preclinical Evaluation of 5F-αMe-3BPA for Improving Pharmacokinetics in Boron Neutron Capture Therapy
by Naoya Kondo, Fuko Hirano, Saki Iritani, Kensuke Suzuki, Anna Miyazaki and Takashi Temma
Pharmaceutics 2026, 18(5), 604; https://doi.org/10.3390/pharmaceutics18050604 - 15 May 2026
Viewed by 262
Abstract
Background/Objectives: Boron neutron capture therapy (BNCT) relies on the selective delivery of boron-10 to tumor cells. Although 4-[10B]borono-L-phenylalanine (BPA) is currently the only clinically approved BNCT agent, it is limited by poor L-type amino acid transporter 1 (LAT1)/LAT2 selectivity and [...] Read more.
Background/Objectives: Boron neutron capture therapy (BNCT) relies on the selective delivery of boron-10 to tumor cells. Although 4-[10B]borono-L-phenylalanine (BPA) is currently the only clinically approved BNCT agent, it is limited by poor L-type amino acid transporter 1 (LAT1)/LAT2 selectivity and aqueous solubility. We previously developed 3-borono-5-fluoro-α-methyl-L-phenylalanine (5F-αMe-3BPA), a novel BPA derivative designed to be a LAT1-targeted BNCT/positron emission tomography theranostic agent. This study comprehensively characterizes its pharmacological profile and explores its pharmacokinetic optimization by modulating renal organic anion transporter 1 (OAT1). Methods: Transport kinetics of BPA, related analogs, and 5F-αMe-3BPA were analyzed in HEK293 cells stably expressing LAT1 or LAT2 using Michaelis–Menten analysis. Time-dependent cellular uptake and intracellular retention of BPA and 5F-αMe-3BPA were evaluated in T3M-4 pancreatic cancer cells with or without the LAT1 inhibitor JPH203. In vivo biodistribution was examined in T3M-4 tumor-bearing mice after intravenous administration of 5F-αMe-3BPA or BPA, with assessment of probenecid pretreatment. Results: 5F-αMe-3BPA retained LAT1 affinity comparable to that of BPA while showing markedly reduced LAT2-mediated transport, indicating improved LAT1/LAT2 selectivity. In T3M-4 cells, 5F-αMe-3BPA showed stronger LAT1 dependence, higher steady-state accumulation, and better intracellular retention than BPA under amino acid-containing conditions. Although 5F-αMe-3BPA achieved favorable tumor-to-plasma and tumor-to-muscle ratios in vivo, it was rapidly cleared from circulation. Probenecid pretreatment increased plasma exposure, reduced early renal accumulation, and significantly enhanced tumor boron accumulation, reaching approximately twofold higher levels than control. Conclusions: These findings establish 5F-αMe-3BPA as a highly LAT1-selective BNCT candidate and identify probenecid pretreatment as a clinically translatable pharmacokinetic strategy for maximizing therapeutic boron delivery. Full article
(This article belongs to the Special Issue Innovative Boron-Based Drug Delivery Systems)
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