A high-boron-loading manganese-based diagnosis and treatment integrated boron medicine and a preparation and application thereof

By designing a high-boron-load manganese-based therapeutic boron drug, utilizing the manganese porphyrin skeleton and catechol borate ester group, the problems of low boron-10 loading and poor blood-brain barrier penetration of boron drugs were solved, enabling precise targeted delivery and real-time imaging monitoring of intracranial tumors, thus improving the efficacy of BNCT treatment.

CN122301925APending Publication Date: 2026-06-30NANTONG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
NANTONG UNIV
Filing Date
2026-03-31
Publication Date
2026-06-30

AI Technical Summary

Technical Problem

The existing BNCT boron drug Boron-10 has a low loading capacity and poor blood-brain barrier penetration, which cannot meet the needs of targeted boron delivery and lesion boron enrichment for refractory solid tumors such as intracranial malignant gliomas, and it also lacks accurate real-time self-monitoring capabilities.

Method used

A high-boron-loading manganese-based therapeutic boron drug was designed, using manganese porphyrin as the core framework and linking boron-10 through catechol borate ester groups to achieve efficient blood-brain barrier penetration. It also has MRI imaging capabilities to achieve real-time dynamic monitoring of boron concentration in tumor tissue.

Benefits of technology

It achieves stable delivery and precise imaging with high boron loading, enabling real-time monitoring of the distribution and metabolism of boron drugs in tumor tissue, thus improving the precision and safety of BNCT treatment.

✦ Generated by Eureka AI based on patent content.

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Abstract

This invention discloses a high-boron-loading manganese-based boron drug for BNCT diagnosis and treatment, its preparation, and its application, belonging to the fields of biomedicine and nuclear medicine. The boron drug structure is shown in general formula 7, with manganese porphyrin as the core skeleton. A benzene ring side chain at the meso position of the porphyrin ring is connected to a boron-10-containing catechol borate ester group via an amide bond. All boron atoms are boron-10 isotopes. The preparation method includes: first constructing the manganese porphyrin skeleton through condensation, cyclization, and metal coordination reactions; then independently preparing boron source units; and finally obtaining the target product through amide bond coupling. This boron drug possesses high boron-10 loading, efficient blood-brain barrier penetration, and excellent MRI imaging performance, enabling real-time and precise monitoring of boron drug distribution in vivo. The quantitative correlation between imaging signals and boron concentration guides the timing of neutron irradiation, integrating MRI tracing and BNCT treatment, effectively solving the problems of low boron loading, inability to penetrate the blood-brain barrier, and difficulty in real-time monitoring of in vivo distribution in existing boron drugs.
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