Intranasal Radioiodinated Ferulic Acid Polymeric Micelles as the First Nuclear Medicine Imaging Probe for ETRA Brain Receptor

Title:Intranasal Radioiodinated Ferulic Acid Polymeric Micelles as the First Nuclear Medicine Imaging Probe for ETRA Brain Receptor

Volume: 17 Issue: 2

Author(s): Hend Fayez, Adli Selim, Rehab Shamma and Hassan Rashed*

Affiliation:

• Department of Labeled Compounds, Hot Laboratories Center, Egyptian Atomic Energy Authority, Cairo, Egypt
• Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Sinai University, Kantara, Egypt

Keywords: Ferulic acid, ¹³¹I, radiolabeling, ETRA receptor, polymeric micelles, imaging probe, nuclear medicine.

Abstract:

Introduction: The aim of this work was to prepare a selective nuclear medicine imaging probe for the Endothelin 1 receptor A in the brain.

Material and Methods: Ferulic acid (an ETRA antagonist) was radiolabeled using ¹³¹I by direct electrophilic substitution method. The radiolabeled ferulic acid was formulated as polymeric micelles to allow intranasal brain delivery. Biodistribution was studied in Swiss albino mice by comparing brain uptake of¹³¹I-ferulic acid after IN administration of ¹³¹I-ferulic acid polymeric micelles, IN administration of ¹³¹I-ferulic acid solution and IV administration of ¹³¹I-ferulic acid solution.

Results: Successful radiolabeling was achieved with an RCY of 98 % using 200 μg of ferulic acid and 60 μg of CAT as oxidizing agents at pH 6, room temperature and 30 min reaction time. ¹³¹I-ferulic acid polymeric micelles were successfully formulated with the particle size of 21.63 nm and polydispersity index of 0.168. Radioactivity uptake in the brain and brain/blood uptake ratio for I.N ¹³¹I-ferulic acid polymeric micelles were greater than the two other routes at all periods.

Conclusion: Our results provide ¹³¹I-ferulic acid polymeric micelles as a hopeful nuclear medicine tracer for ETRA brain receptor.

Cite this article as:

Fayez Hend, Selim Adli, Shamma Rehab and Rashed Hassan*, Intranasal Radioiodinated Ferulic Acid Polymeric Micelles as the First Nuclear Medicine Imaging Probe for ETRA Brain Receptor, Current Radiopharmaceuticals 2024; 17 (2) . https://dx.doi.org/10.2174/0118744710269885231113070356