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F-18-labeling syntheses and preclinical evaluation of functionalized nanoliposomes for Alzheimer's disease
- Source :
- European Journal of Pharmaceutical Sciences. 88:257-266
- Publication Year :
- 2016
-
Abstract
- The aim of the present study was to synthesize functionalized (18)F-labeled NLs ((18)F-NLs) and evaluate their biological behavior in mouse models of Alzheimer's disease (AD) using positron emission tomography (PET) and ex vivo brain autoradiography. (18)F-fluorine was introduced to (18)F-NLs either by using a core forming (18)F-lipid or by encapsulating a (18)F-tracer, (18)F-treg-curcumin inside the NLs. Phosphatidic acid (PA) and curcumin derivative (Curc) functionalized (18)F-NLs with or without additional mApoE functionalization were produced using thin film hydration. The biodistribution and β-amyloid plaque-binding ability of (18)F-NLs were studied in wild type mice and AD mouse models using in vivo PET imaging and ex vivo brain autoradiography at 60min after (18)F-NL injection. Functionalized (18)F-NLs were successfully synthesized. The preclinical evaluation in mice showed that the functional group affected the biodistribution of (18)F-NLs. Further functionalization with mApoE increased the brain-to-blood ratio of (18)F-NLs but the overall brain uptake remained low with all functionalized (18)F-NLs. The liposomal encapsulation of (18)F-treg-curcumin was not successful and preclinical results of encapsulated (18)F-treg-curcumin and plain (18)F-treg-curcumin were identical. Although the studied functionalized (18)F-NLs were not suitable for PET imaging as such, the synthesis techniques introduced in this study can be utilized to modify the biological behavior of (18)F-labeled NLs.
- Subjects :
- Male
0301 basic medicine
Fluorine Radioisotopes
Pathology
Pharmaceutical Science
02 engineering and technology
environment and public health
Mice
chemistry.chemical_compound
Tissue Distribution
ta317
Liposome
Molecular Structure
medicine.diagnostic_test
Genes, Transgenic, Suicide
Brain
Phosphatidic acid
Alzheimer's disease
021001 nanoscience & nanotechnology
Positron emission tomography
Positron emission tomography (PET)
Female
0210 nano-technology
Nucleophilic 18F-fluorination
Biodistribution
medicine.medical_specialty
β-amyloid plaques
β-amyloid plaque
ta3112
03 medical and health sciences
Alzheimer Disease
In vivo
Functionalized nanoliposome
medicine
Animals
Technology, Pharmaceutical
NLS
business.industry
Fluorine
Nanostructures
030104 developmental biology
chemistry
Positron-Emission Tomography
Liposomes
Biophysics
Curcumin
Autoradiography
Radiopharmaceuticals
business
Ex vivo
Subjects
Details
- Language :
- English
- ISSN :
- 09280987
- Volume :
- 88
- Database :
- OpenAIRE
- Journal :
- European Journal of Pharmaceutical Sciences
- Accession number :
- edsair.doi.dedup.....d60db02499b6fe39b34a28886c9102dd