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Radioiodination, nasal nanoformulation and preliminary evaluation of isovanillin: A new potential brain
O A El-Kawy1, H A Shweeta1, K M Attallah1
1Egyptian Atomic Energy Authority, Labelled Compounds Department, 13759, Cairo, Egypt.
Abstract:
Brain cancer is a challenging disease to treat using conventional approaches. The present investigation aimed to develop a radiopharmaceutical targeting brain cancer based on natural isovanillin. Different parameters were optimized, resulting in high radiolabeling efficiency (97.3 ± 1.2%) and good stability (<48 h). The tracer was formulated for intranasal delivery in a chitosan nanoparticles system with a mean particle size of 141 ± 2 nm, a polydispersity index of 0.23 ± 0.02, and a zeta potential of -17.4 ± 0.3 mV to enhance nasal uptake and surmount the blood-brain barrier. The system was characterized and assessed in-vitro for suitability and specificity and evaluated in-vivo in normal and tumorized mice. The biodistribution profile in brain tumor showed 20.5 ± 0.4 %ID/g localization and cancer cell targeting within 60 min. Improvement in brain tumor uptake resulted from both the nanoformulation and nasal administration of iodoisovanillin. Overall, the reported results encourage the potential use of the nanoformulated labeled compound as an anticancer agent.
Insights
Researchers developed a novel radiopharmaceutical from natural isovanillin for brain cancer. This nanoformulated tracer, delivered intranasally, effectively targets brain tumors, offering a promising new anticancer strategy.
Area of Science:
- Radiopharmaceutical development
- Nanomedicine
- Oncology
Background:
- Brain cancer presents significant treatment challenges with conventional methods.
- Targeted drug delivery across the blood-brain barrier remains a hurdle.
- Natural compounds offer potential for novel therapeutic agents.
Purpose of the Study:
- To develop a novel radiopharmaceutical for brain cancer targeting using natural isovanillin.
- To formulate the radiotracer for enhanced intranasal delivery and blood-brain barrier penetration.
- To evaluate the in vitro and in vivo efficacy of the nanoformulated radiotracer.
Main Methods:
- Optimization of radiolabeling parameters for isovanillin.
- Formulation of the radiotracer in chitosan nanoparticles for intranasal delivery.
- In vitro characterization and specificity assessment.
- In vivo biodistribution studies in normal and tumor-bearing mice.
Main Results:
- High radiolabeling efficiency (97.3 ± 1.2%) and stability (<48 h) achieved.
- Chitosan nanoparticles exhibited optimal characteristics (141 ± 2 nm size, 0.23 ± 0.02 PDI, -17.4 ± 0.3 mV zeta potential).
- Significant brain tumor uptake (20.5 ± 0.4 %ID/g) and cancer cell targeting within 60 min demonstrated in vivo.
- Intranasal administration and nanoformulation enhanced tumor localization.
Conclusions:
- The developed nanoformulated iodoisovanillin shows potential as an effective radiopharmaceutical for brain cancer.
- Intranasal delivery combined with nanotechnology enhances brain tumor targeting.
- This approach offers a promising strategy for brain cancer treatment and diagnosis.
