Repurposing radiopharmaceutical carriers for targeted drug delivery and theranostics: A translational framework.
Repurposing radiopharmaceutical carriers for drug delivery could accelerate precision therapeutics, but challenges remain in bridging diagnostic and therapeutic applications.
Where it sits
this study against the rest of the octreotide corpusSummary and findings
This review discusses the potential of repurposing radiopharmaceutical carriers for targeted drug delivery and theranostics. It focuses on clinically validated carriers such as peptides and antibody fragments. The paper highlights the integration of classical radiopharmaceutical principles with recent advances to enhance therapeutic delivery.
Abstract
Radiopharmaceuticals have long demonstrated precise, organ- and receptor-specific targeting in humans, supported by well-characterized pharmacokinetics, standardized formulation, and regulatory validation; however, the carrier systems underlying these agents remain largely underexplored as platforms for therapeutic delivery. This review introduces a translational framework that repositions clinically validated radiopharmaceutical carriers, including peptides, nanocolloids, lipophilic complexes, and antibody fragments, as ready-to-deploy scaffolds for targeted drug delivery and theranostic applications. Integrating classical radiopharmaceutical principles with advances from 2018 to 2025, this work examines how established systems based on technetium-99m (<sup>99</sup>ᵐTc), gallium, lutetium, rhenium, copper, iodine, and actinium can be systematically re-engineered through linker design, bifunctional chelation, and payload integration. Unlike conventional nanocarriers that rely heavily on preclinical optimization and passive targeting mechanisms, these platforms offer pre-validated human biodistribution, reproducible pharmacokinetics, and compatibility with good manufacturing practice (GMP), providing a distinct advantage for clinical translation. Emerging clinical evidence, including peptide-drug conjugates and antibody-based systems, highlights both the feasibility and current limitations of this approach, particularly the gap between diagnostic success and therapeutic adaptation. By integrating mechanistic insights, design strategies, and translational considerations, this review proposes a shift from de novo carrier design toward the strategic repurposing of clinically proven systems, with the potential to reduce translational attrition and accelerate the development of precision therapeutics and next-generation theranostic platforms.
Background
Radiopharmaceuticals have long been used for precise targeting in diagnostic imaging, but their potential as carriers for therapeutic delivery remains underexplored. This study addresses the possibility of repurposing these carriers, which have established pharmacokinetics and regulatory validation, for drug delivery and theranostic applications. The research is significant as it proposes a framework that could reduce translational attrition and accelerate precision therapeutics development.
Methods
This is a review article that synthesizes existing literature and clinical evidence from 2018 to 2025. It examines the use of radiopharmaceutical carriers, including peptides and antibody fragments, for targeted drug delivery. The review integrates classical radiopharmaceutical principles with recent advances in linker design, bifunctional chelation, and payload integration.
Results
Not reported in abstract.
Interpretation
The review suggests that repurposing radiopharmaceutical carriers could offer advantages over conventional nanocarriers due to their pre-validated human biodistribution and pharmacokinetics. However, the gap between diagnostic success and therapeutic adaptation remains a challenge. The proposed framework could potentially streamline the development of precision therapeutics, though clinical evidence is still emerging.
Key findings
- Radiopharmaceuticals demonstrate precise organ- and receptor-specific targeting.
- Carriers include peptides, nanocolloids, lipophilic complexes, and antibody fragments.
- Technetium-99m, gallium, lutetium, rhenium, copper, iodine, and actinium are key elements.
- Platforms offer pre-validated human biodistribution and reproducible pharmacokinetics.
- Emerging clinical evidence highlights feasibility and limitations of this approach.
Limitations
- Review article, no new experimental data
- Gap between diagnostic success and therapeutic adaptation
- Lack of specific quantitative outcomes
- Emerging clinical evidence, not fully established