99mTc Stearyl 6-(benzylidenehydrazinyl) nicotinamide Liposomes as Tumor Permeability Evaluation Tracer
| Autor: | Williams Porcal, Mirel Cabrera, Pablo Cabral, Marcelo Fernández, Nicole Lecot, Juan Pablo Gambini |
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| Rok vydání: | 2021 |
| Předmět: |
Biodistribution
Pharmaceutical Science 02 engineering and technology Aquatic Science Pharmacology 030226 pharmacology & pharmacy 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine In vivo Drug Discovery medicine Ecology Evolution Behavior and Systematics Liposome Ecology Nicotinamide Melanoma General Medicine 021001 nanoscience & nanotechnology medicine.disease chemistry Permeability (electromagnetism) Nanomedicine Nanocarriers 0210 nano-technology Agronomy and Crop Science |
| Zdroj: | AAPS PharmSciTech. 22 |
| ISSN: | 1530-9932 |
| DOI: | 10.1208/s12249-021-01984-1 |
| Popis: | Nanomedicine is a highly demanded discipline. Liposomes have seen an increased attention due to their physicochemical properties that allow them to act as nanocarriers of drugs and also of radioisotopes that can be used to diagnose and treat cancer. In order to obtain a novel permeability cancer imaging agent based on 99mTc-labeled liposomes, we describe microwave-assisted synthesis of stearyl 6-(benzylidenehydrazinyl) nicotinamide lipid, which was included in two formulations: nanometric hydrazinonicotinic acid (HYNIC) liposome and its PEGylated coated analogue, HYNIC-PEG liposome. Radiolabeling with 99mTc via stearyl 6-(benzylidenehydrazinyl) nicotinamide was found to be easy, reproducible, and stable, revealing high radiochemical purity (94 ± 1.7%) for both liposomal formulations. Biodistribution at 4 h and 24 h and scintigraphic images at 4 h were performed in normal and melanoma-bearing C57BL/6 mice. Biodistribution studies at 4 h showed tumor uptake of 99mTc-HYNIC liposome and 99mTc-HYNIC-PEG liposome (1.1 ± 0.6 and 2.5 ± 0.4, respectively) and also at 24 h p.i. (1.8 ± 0.5 and 3.0 ± 1.1, respectively). Scintigraphic images showed appreciable tumor uptake in melanoma tumor-bearing mice with both liposomal formulations. Our results show that 99mTc stearyl 6-(benzylidenehydrazinyl) nicotinamide liposomes can be used as diagnostic noninvasive in vivo tumor-targeting agents capable of evaluating tumor permeability and development who can be used in personalized chemotherapy planning. |
| Databáze: | OpenAIRE |
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