Synthesis and Characterization of a “Clickable” PBR28 TSPO-Selective Ligand Derivative Suitable for the Functionalization of Biodegradable Polymer Nanoparticles

Auriemma, Renato; Sponchioni, Mattia; Palmiero, Umberto Capasso; Rossino, Giacomo; Rossetti, Arianna; Marsala, Andrea; Collina, Simona; Sacchetti, Alessandro; Moscatelli, Davide; Peviani, Marco

doi:10.3390/nano11071693

Cited by 4 publications

(4 citation statements)

References 31 publications

(51 reference statements)

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“…5b). Fluorescence emission plot of MCBP with BSA at different concentrations of MCBP (9,17,25,33,41,49, 57 mM) (here L represents MCBP).…”

Section: Molecular Dockingmentioning

confidence: 99%

“…[23][24][25][26][27][28][29] Although many new TSPO ligands have been synthesized, only a few of them contain groups that may be derivatized, making them appropriate for the creation of targeted nanocarriers that can deliver therapeutics and diagnostics to mitochondria. [30][31][32][33][34][35][36][37][38][39][40][41][42] One of the top choices among radioisotopes utilized in SPECT imaging is 99m Tc, largely attributed to its optimal radio-tracer characteristics. With a low radiation burden of 140 keV and a suitable half-life of 6 hours, it stands out as an ideal option.…”

Section: Introductionmentioning

confidence: 99%

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An 18 kDa TSPO specific ligand-based polymeric nanoformulation: synthesis, computational and biological studies

Singh,

Kakkar

et al. 2024

New J. Chem.

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“…5b). Fluorescence emission plot of MCBP with BSA at different concentrations of MCBP (9,17,25,33,41,49, 57 mM) (here L represents MCBP).…”

Section: Molecular Dockingmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

An 18 kDa TSPO specific ligand-based polymeric nanoformulation: synthesis, computational and biological studies

Singh,

Kakkar

et al. 2024

New J. Chem.

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“…The residues of propargylamine exhibited neuroprotective effects resembling the effect of neuroprotective drugs such as Rasagiline ( Amit et al, 2017 ). Auriemma et al (2021) used CuAAC to decorate zwitterionic PCL-based nanoparticles with a radioligand (PBR28 derivative) selective for the 18 kDa translocator protein (TSPO), which is highly upregulated in the brain in pathological conditions. In this way, the authors assessed and monitored the microgliosis.…”

Section: Polymer Functionalization Strategiesmentioning

confidence: 99%

Functionalization strategies of polymeric nanoparticles for drug delivery in Alzheimer’s disease: Current trends and future perspectives

et al. 2022

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Alzheimer’s disease (AD), the most common form of dementia, is a progressive and multifactorial neurodegenerative disorder whose primary causes are mostly unknown. Due to the increase in life expectancy of world population, including developing countries, AD, whose incidence rises dramatically with age, is at the forefront among neurodegenerative diseases. Moreover, a definitive cure is not yet within reach, imposing substantial medical and public health burdens at every latitude. Therefore, the effort to devise novel and effective therapeutic strategies is still of paramount importance. Genetic, functional, structural and biochemical studies all indicate that new and efficacious drug delivery strategies interfere at different levels with various cellular and molecular targets. Over the last few decades, therapeutic development of nanomedicine at preclinical stage has shown to progress at a fast pace, thus paving the way for its potential impact on human health in improving prevention, diagnosis, and treatment of age-related neurodegenerative disorders, including AD. Clinical translation of nano-based therapeutics, despite current limitations, may present important advantages and innovation to be exploited in the neuroscience field as well. In this state-of-the-art review article, we present the most promising applications of polymeric nanoparticle-mediated drug delivery for bypassing the blood-brain barrier of AD preclinical models and boost pharmacological safety and efficacy. In particular, novel strategic chemical functionalization of polymeric nanocarriers that could be successfully employed for treating AD are thoroughly described. Emphasis is also placed on nanotheranostics as both potential therapeutic and diagnostic tool for targeted treatments. Our review highlights the emerging role of nanomedicine in the management of AD, providing the readers with an overview of the nanostrategies currently available to develop future therapeutic applications against this chronic neurodegenerative disease.

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“…Poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) can contribute to both effects simultaneously due to its zwitterionic nature and has provided extensive evidence of high stability in biological fluids, biocompatibility, and low immunogenicity compared to classic poly(ethylene glycol) (PEG). − In addition, incorporating hydrophobic chains would allow the particles to encapsulate water–insoluble drugs that are later released according to time or specific stimuli. , Another critical feature of the theranostic platform is the biodegradability to eliminate it after achieving the therapeutic goal. Amphiphilic copolymers comprising a hydrophilic block and a hydrophobic segment based on ε-caprolactone (CL) have proven effective in these requirements. − An ideal strategy to obtain a polymer with these combined characteristics is the reversible addition–fragmentation chain transfer (RAFT) polymerization that allows great control over the design of the polymer microstructure and, thus, engineers the material for the desired applications. , …”

Section: Introductionmentioning

confidence: 99%

Magnetite Nanoparticles Coated with Biodegradable Zwitterionic Polymers as Multifunctional Nanocomposites for Drug Delivery and Cancer Treatment

Perecin

Sponchioni

Auriemma

et al. 2022

ACS Appl. Nano Mater.

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Tailor-made materials for biomedical applications can be constructed with different building blocks to confer multiple functions on one platform. Here, we demonstrate the facile synthesis of magnetite-biodegradable polymer nanocomposites combining superparamagnetism with the possibility of loading and controlling the release of a lipophilic drug. The magnetite nanoparticles were synthesized by reduction–precipitation and used as nuclei to grow a biodegradable zwitterionic shell. The copolymer used for this scope comprises a hydrophobic block made of a biodegradable ε-caprolactone-based macromonomer (CL n ) with three different degrees of polymerization (DP n , n = 3, 5, and 7) obtained by ring-opening polymerization (ROP). Dopamine molecules were attached to the end of this CL n oligomer (CL n Dopa), conferring a specific affinity for the magnetite surface. A hydrophilic zwitterionic poly(2-methacryloyloxyethyl phosphorylcholine) block (PMPC) was included by reversible addition–fragmentation chain transfer (RAFT) polymerization to add colloidal stability and water dispersibility to the copolymer. This PMPC was chain-extended with CL n Dopa via RAFT polymerization targeting four different DP m (m = 10, 20, 30, and 40), resulting in a library of 12 copolymers. A facile nanoprecipitation process produced copolymer nanoparticles and copolymer-coated magnetite nanostructures. Physicochemical characterization confirmed the inorganic–organic composite nature. The copolymer-coated magnetic materials showed water stability, superparamagnetic behavior, and appropriate hyperthermic ability under an alternate magnetic field. Biological assays using HeLa cells showed high biocompatibility and efficient nanoparticle uptake. In addition, a sustained release of dexamethasone, used as a model drug encapsulated in the polymer shell, and local heating as a dual functional material could be accessed.

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Synthesis and Characterization of a “Clickable” PBR28 TSPO-Selective Ligand Derivative Suitable for the Functionalization of Biodegradable Polymer Nanoparticles

Cited by 4 publications

References 31 publications

An 18 kDa TSPO specific ligand-based polymeric nanoformulation: synthesis, computational and biological studies

An 18 kDa TSPO specific ligand-based polymeric nanoformulation: synthesis, computational and biological studies

Functionalization strategies of polymeric nanoparticles for drug delivery in Alzheimer’s disease: Current trends and future perspectives

Magnetite Nanoparticles Coated with Biodegradable Zwitterionic Polymers as Multifunctional Nanocomposites for Drug Delivery and Cancer Treatment

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