Function Oriented Molecular Design: Dendrimers as Novel Antimicrobials

García‐Gallego, Sandra; Franci, Gianluigi; Falanga, Annarita; Gómez, Rafael; Folliero, Veronica; Galdiero, Stefania; Mata, Francisco de la; Galdiero, Massimiliano

doi:10.3390/molecules22101581

Cited by 53 publications

(54 citation statements)

References 172 publications

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“…The dendrimers themselves possess their own antimicrobial activity, demonstrated by numerous studies [ 192 , 193 ]. The most used dendrimeric polymers in various therapeutic applications are the PAMAM and PPI dendrimers [ 194 ]. Due to the multifunctional groups in the structure of dendrimers, they can be conjugated with antibiotics, thus enhancing the activity of both compounds.…”

Section: Biomedical Applications Of Dendrimersmentioning

confidence: 99%

Applications and Limitations of Dendrimers in Biomedicine

et al. 2020

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Biomedicine represents one of the main study areas for dendrimers, which have proven to be valuable both in diagnostics and therapy, due to their capacity for improving solubility, absorption, bioavailability and targeted distribution. Molecular cytotoxicity constitutes a limiting characteristic, especially for cationic and higher-generation dendrimers. Antineoplastic research of dendrimers has been widely developed, and several types of poly(amidoamine) and poly(propylene imine) dendrimer complexes with doxorubicin, paclitaxel, imatinib, sunitinib, cisplatin, melphalan and methotrexate have shown an improvement in comparison with the drug molecule alone. The anti-inflammatory therapy focused on dendrimer complexes of ibuprofen, indomethacin, piroxicam, ketoprofen and diflunisal. In the context of the development of antibiotic-resistant bacterial strains, dendrimer complexes of fluoroquinolones, macrolides, beta-lactamines and aminoglycosides have shown promising effects. Regarding antiviral therapy, studies have been performed to develop dendrimer conjugates with tenofovir, maraviroc, zidovudine, oseltamivir and acyclovir, among others. Furthermore, cardiovascular therapy has strongly addressed dendrimers. Employed in imaging diagnostics, dendrimers reduce the dosage required to obtain images, thus improving the efficiency of radioisotopes. Dendrimers are macromolecular structures with multiple advantages that can suffer modifications depending on the chemical nature of the drug that has to be transported. The results obtained so far encourage the pursuit of new studies.

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Section: Biomedical Applications Of Dendrimersmentioning

confidence: 99%

Applications and Limitations of Dendrimers in Biomedicine

et al. 2020

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“…The idea came from dendrimeric peptides, small nanosystems with a size range from 2 to 50 nm, with great advantages in terms of biocompatibility, structural/functional versatility and drug delivery efficiency (Tam, 1988 ; Tam et al, 2002 ; Serna et al, 2017 ). These systems are characterized by a hyper-branched and almost perfect geometrical 3D architecture, that grow from the core into a globular shape, with reported activity against infectious pathogens and cancer cells (Tam et al, 2002 ; Ionov et al, 2013 ; García-Gallego et al, 2017 ). Examples of systems already studied are diverse, with each author exploring different mechanisms to promote the assembling or activity toward the target cells.…”

Section: Nanoparticles In Therapeuticsmentioning

confidence: 99%

Application of Light Scattering Techniques to Nanoparticle Characterization and Development

et al. 2018

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Over the years, the scientific importance of nanoparticles for biomedical applications has increased. The high stability and biocompatibility, together with the low toxicity of the nanoparticles developed lead to their use as targeted drug delivery systems, bioimaging systems, and biosensors. The wide range of nanoparticles size, from 10 nm to 1 μm, as well as their optical properties, allow them to be studied using microscopy and spectroscopy techniques. In order to be effectively used, the physicochemical properties of nanoparticle formulations need to be taken into account, namely, particle size, surface charge distribution, surface derivatization and/or loading capacity, and related interactions. These properties need to be optimized considering the final nanoparticle intended biodistribution and target. In this review, we cover light scattering based techniques, namely dynamic light scattering and zeta-potential, used for the physicochemical characterization of nanoparticles. Dynamic light scattering is used to measure nanoparticles size, but also to evaluate their stability over time in suspension, at different pH and temperature conditions. Zeta-potential is used to characterize nanoparticles surface charge, obtaining information about their stability and surface interaction with other molecules. In this review, we focus on nanoparticle characterization and application in infection, cancer and cardiovascular diseases.

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“…Several unique properties associated with dendrimers allows them to be used in many applications such as catalysis [ 11 , 12 , 13 , 14 ], sensing [ 15 , 16 , 17 ], and fluorescence applications [ 18 , 19 , 20 , 21 , 22 ], General synthesis routes to these dendrimers involve functionalizing the periphery with antimicrobial agents [ 6 ]. The search for unique synthesis approaches of antimicrobial dendrimers is expanding with the focus on enhanced activity upon resistant strains [ 15 , 16 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 ]. The advantage of including η 6 -aryl-η 5 -cyclopentadienyliron (II) complexes into dendritic structures is to provide highly-ordered structures with engaging bioactivity and other properties [ 16 , 37 , 38 ].…”

Section: Introductionmentioning

confidence: 99%

Design of Organoiron Dendrimers Containing Paracetamol for Enhanced Antibacterial Efficacy

2020

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Paracetamol (acetaminophen) is a common painkiller and antipyretic drug used globally. Attachment of paracetamol to a series of organoiron dendrimers was successfully synthesized. The aim of this study is to combine the benefits of the presence of these redox-active organoiron dendrimers, their antimicrobial activities against some human pathogenic Gram-positive, and the therapeutic characteristics of paracetamol. The antimicrobial activity of these dendrimers was investigated and tested with a minimum inhibitory concentration and this has been reported. Some of these newly synthesized dendrimers exhibited the highest inhibitory activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium (VRE), and Staphylococcus warneri compared to reference drugs. The results of this study indicate that the antimicrobial efficacy of the dendrimers is dependent on the size of the redox-active organoiron dendrimer and its terminal functionalities. The best result has been recorded for the fourth-generation dendrimer 11, which attached to 48 paracetamol end groups and has 90 units composed of the η6-aryl-η5-cyclopentadienyliron (II) complex. This dendrimer presented inhibition of 50% of the growth (IC50) of 0.52 μM for MRSA, 1.02 μM for VRE, and 0.73 μM for Staphylococcus warneri. The structures of the dendrimers were characterized by elemental analysis, Fourier transform infrared (FT-IR), nuclear magnetic resonance (1H-NMR), and 13C-NMR spectroscopic techniques. In addition, all synthesized dendrimers displayed good thermal stability in the range of 300–350 °C following the degradation of the cationic iron moieties which occurred around 200 °C.

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Function Oriented Molecular Design: Dendrimers as Novel Antimicrobials

Cited by 53 publications

References 172 publications

Applications and Limitations of Dendrimers in Biomedicine

Applications and Limitations of Dendrimers in Biomedicine

Application of Light Scattering Techniques to Nanoparticle Characterization and Development

Design of Organoiron Dendrimers Containing Paracetamol for Enhanced Antibacterial Efficacy

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