EXCI-CEST: Exploiting pharmaceutical excipients as MRI-CEST contrast agents for tumor imaging
| Autor: | Lorena Consolino, Alexandre Zerbo, Annasofia Anemone, Fatima Zzahra Moustaghfir, Dario Livio Longo, Silvio Aime, Martina Bracesco |
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| Rok vydání: | 2017 |
| Předmět: |
Drug
Stereochemistry Chemical exchange saturation transfer media_common.quotation_subject Contrast Media Pharmaceutical Science Imaging 030218 nuclear medicine & medical imaging Excipients Mice 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Nuclear magnetic resonance Neoplasms Amide medicine Animals Contrast (vision) Inbred BALB C media_common Tumor imaging CEST MRI Tumor Algorithms Female Mice Inbred BALB C Protons Xenograft Model Antitumor Assays Magnetic Resonance Imaging 3003 medicine.diagnostic_test Meglumine Chemistry Magnetic resonance imaging Ascorbic acid 3. Good health Saturation transfer 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | International journal of pharmaceutics 525 (2017): 275–281. doi:10.1016/j.ijpharm.2017.04.040 info:cnr-pdr/source/autori:Longo, Dario Livio; Moustaghfir, Fatima Zzahra; Zerbo, Alexandre; Consolino, Lorena; Anemone, Annasofia; Bracesco, Martina; Aime, Silvio/titolo:EXCI-CEST: Exploiting pharmaceutical excipients as MRI-CEST contrast agents for tumor imaging/doi:10.1016%2Fj.ijpharm.2017.04.040/rivista:International journal of pharmaceutics (Print)/anno:2017/pagina_da:275/pagina_a:281/intervallo_pagine:275–281/volume:525 International Journal of Pharmaceutics |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/j.ijpharm.2017.04.040 |
| Popis: | Chemical Exchange Saturation Transfer (CEST) approach is a novel tool within magnetic resonance imaging (MRI) that allows visualization of molecules possessing exchangeable protons with water. Many molecules, employed as excipients for the formulation of finished drug products, are endowed with hydroxyl, amine or amide protons, thus can be exploitable as MRI-CEST contrast agents. Their high safety profiles allow them to be injected at very high doses. Here we investigated the MRI-CEST properties of several excipients (ascorbic acid, sucrose, N-acetyl-D-glucosamine, meglumine and 2-pyrrolidone) and tested them as tumor-detecting agents in two different murine tumor models (breast and melanoma cancers). All the investigated molecules showed remarkable CEST contrast upon i.v. administration in the range 1-3 ppm according to the type of mobile proton groups. A marked increase of CEST contrast was observed in tumor regions up to 30 min post injection. The combination of marked tumor contrast enhancement and lack of toxicity make these molecules potential candidates for the diagnosis of tumors within the MRI-CEST approach. (C) 2017 Elsevier B.V. All rights reserved. |
| Databáze: | OpenAIRE |
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