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Antibacterial Activity Of Antipsychotic Agents, Their Association With Lipid Nanocapsules And Its Impact On The Properties Of The Nanocarriers And On Antibacterial Activity

H. Nehme, P. Saulnier, A. Ramadan, V. Cassisa, C. Guillet, M. Eveillard, A. Umerska
Published 2018 · Chemistry, Medicine

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Bacterial antibiotic resistance is an emerging public health problem worldwide; therefore, new therapeutic strategies are needed. Many studies have described antipsychotic compounds that present antibacterial activity. Hence, the aims of this study were to evaluate the in vitro antibacterial activity of antipsychotics belonging to different chemical families, to assess the influence of their association with lipid nanocapsules (LNCs) on their antimicrobial activity as well as drug release and to study the uptake of LNCs by bacterial cells. Antibacterial activity was evaluated against Gram-positive Staphylococcus aureus and Gram negative Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Acinetobacter baumannii by minimum inhibitory concentration (MIC) assay, and the capability of killing tested microorganisms was evaluated by time kill assay. LNCs were prepared by phase inversion method, and the antipsychotic agents were incorporated using pre-loading and post-loading strategies. Only phenothiazines and thioxanthenes showed antibacterial activity, which was independent of antibiotic-resistance patterns. Loading the nanocarriers with the drugs affected the properties of the former, particularly their zeta potential. The release rate depended on the drug and its concentration—a maximum of released drug of less than 40% over 24 hours was observed for promazine. The influence of the drug associations on the antibacterial properties was concentration-dependent since, at low concentrations (high nanocarrier/drug ratio), the activity was lost, probably due to the high affinity of the drug to nanocarriers and slow release rate, whereas at higher concentrations, the activity was well maintained for the majority of the drugs. Chlorpromazine and thioridazine increased the uptake of the LNCs by bacteria compared with blank LNCs, even below the minimum inhibitory concentration.
This paper references
Triflupromazine : a microbicide nonantibiotic compound
SG Dastidar (2004)
Chondroitin-based nanoplexes as peptide delivery systems--Investigations into the self-assembly process, solid-state and extended release characteristics.
A. Umerska (2015)
Search of antimicrobial activity of selected non-antibiotic drugs.
H. Kruszewska (2002)
Cubosomes post-loaded with antimicrobial peptides: characterization, bactericidal effect and proteolytic stability.
Lukas Boge (2017)
Lipid-Based Liquid Crystals As Carriers for Antimicrobial Peptides: Phase Behavior and Antimicrobial Effect.
Lukas Boge (2016)
Formulation and nebulization of fluticasone propionate-loaded lipid nanocarriers.
A. Umerska (2015)
Liposome - Encapsulated Antibiotics 1
In vitro and in vivo antimycobacterial activity of an antihypertensive agent methylL - DOPA
NK Dutta (2005)
Antibacterial activity of the antiinflammatory agent diclofenac sodium.
S. Annadurai (1998)
Thioridazine: resurrection as an antimicrobial agent?
H. K. R. Thanacoody (2007)
Multicomponent drug efflux complexes: architecture and mechanism of assembly.
H. Zgurskaya (2009)
Synergistic interactions between doxycycline and terpenic components of essential oils encapsulated within lipid nanocapsules against gram negative bacteria.
C. Valcourt (2016)
Synergistic interactions between antimicrobial peptides derived from plectasin and lipid nanocapsules containing monolaurin as a cosurfactant against Staphylococcus aureus
A. Umerska (2017)
The future of antibiotics and resistance: a tribute to a career of leadership by John Bartlett.
B. Spellberg (2014)
Understanding the adsorption of salmon calcitonin, antimicrobial peptide AP114 and polymyxin B onto lipid nanocapsules.
A. Umerska (2016)
Lipid nanoparticles for the delivery of poorly water‐soluble drugs
H. Bunjes (2010)
Antibacterial effect of some phenothiazine compounds and R-factor elimination by chlorpromazine.
J. Molnár (1976)
In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates
Moustafa A. El-Nakeeb (2011)
A Novel Phase Inversion-Based Process for the Preparation of Lipid Nanocarriers
B. Heurtault (2004)
Antibacterial Activity of Artificial Phenothiazines and Isoflavones from Plants
A. Dasgupta (2008)
Trifluoperazine: a broad spectrum bactericide especially active on staphylococci and vibrios.
R. Mazumder (2001)
Activity of aminoglycosides, including ACHN-490, against carbapenem-resistant Enterobacteriaceae isolates.
D. Livermore (2011)
Antibiotic-eluting medical devices for various applications.
M. Zilberman (2008)
In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates
Moustafa A. El-Nakeeb (2011)
Lipid nanocapsules: a new platform for nanomedicine.
N. Huynh (2009)
Triflupromazine: a microbicide non-antibiotic compound.
S. Dastidar (2004)
Multidrug efflux pumps of gram-negative bacteria.
H. Nikaido (1996)
Treatment and Prevention of Urinary Tract Infection with Orally Active FimH Inhibitors
C. K. Cusumano (2011)
Antibacterial action of lipid nanocapsules containing fatty acids or monoglycerides as co-surfactants.
A. Umerska (2016)
In vitro and in vivo antimicrobial action of fluphenazine.
S. Dastidar (1995)
Persistence of nasal colonization with human pathogenic bacteria and associated antimicrobial resistance in the German general population
R. Köck (2016)
Tetracycline delivery from fibrin controls peritoneal infection without measurable systemic antibiotic.
C. Woolverton (2001)
Synergistic interactions between antimicrobial peptides derived from plectasin and lipid nanocapsules containing monolaurin as a co - surfactant against Staphylococcus aureus
A Umerska (2017)
Liposome-encapsulated antibiotics.
I. Salem (2005)
Outer membrane of salmonella. Sites of export of newly synthesised lipopolysaccharide on the bacterial surface.
P. Mühlradt (1973)
Activity of Plazomicin (ACHN-490) against MDR clinical isolates of Klebsiella pneumoniae, Escherichia coli, and Enterobacter spp. from Athens, Greece
I. Galani (2012)
Role of Phenothiazines and Structurally Similar Compounds of Plant Origin in the Fight against Infections by Drug Resistant Bacteria
S. Dastidar (2013)
Interaction of two phenothiazine derivatives with phospholipid monolayers.
A. Hidalgo (2004)
Outer membrane permeability and antibiotic resistance.
A. Delcour (2009)
Molecular Basis of Bacterial Outer Membrane Permeability Revisited
H. Nikaido (2003)
Outer membranes of Gram‐negative bacteria are permeable to steroid probes
P. Plésiat (1992)
In vitro and in vivo antimycobacterial activity of an antihypertensive agent methyl-L-DOPA.
N. Dutta (2005)
Self-assembled hyaluronate/protamine polyelectrolyte nanoplexes: synthesis, stability, biocompatibility and potential use as peptide carriers.
A. Umerska (2014)
Surface active properties of lipid nanocapsules
C. R. Mouzouvi (2017)

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M. Seeman (2021)
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Maytham Hussein (2020)
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T. Ronco (2020)
Nitric oxide-releasing cyclodextrins as biodegradable antibacterial scaffolds: a patent evaluation of US2019343869(A1).
M. Pieroni (2020)
Schizophrenia and the microbiome: Time to focus on the impact of antipsychotic treatment on the gut microbiota
T. Dinan (2018)
Gut microbes in neurocognitive and mental health disorders
T. Halverson (2020)
Intracellular availability of poorly soluble drugs from lipid nanocapsules
Marilena S Bohley (2019)
Elucidation of the crystal structure of FabD from the multidrug-resistant bacterium Acinetobacter baumannii.
W. C. Lee (2018)
Aripiprazole repurposed as an inhibitor of biofilm formation, and sterol biosynthesis in multi-drug resistant Candida albicans.
S. K. Rajasekharan (2019)
A Novel Derivative of Thioridazine Shows Low Toxicity and Efficient Activity against Gram-Positive Pathogens
Nadia S. Jørgensen (2020)
Screening and identification of Aspergillus activity against Xanthomonas oryzae pv. oryzae and analysis of antimicrobial components
B. Jiang (2019)
Nanoscience in Medicine Vol. 1
Hemant Kumar Daima (2020)
Polymeric Nanoparticles for Increasing Oral Bioavailability of Curcumin
A. Umerska (2018)
The Other Obesity Epidemic—Of Drugs and Bugs
Adonis Sfera (2020)
Effective targeted therapy for drug-resistant infection by ICAM-1 antibody-conjugated TPGS modified β-Ga2O3:Cr3+ nanoparticles
Xu-Qi Kang (2019)
Dos distúrbios psiquiátricos à antibioticoterapia: reposicionamento da clorpromazina como agente antibacteriano
W. Lima (2019)
Do phenothiazines possess antimicrobial and efflux inhibitory properties?
Elizabeth M Grimsey (2019)
Antimicrobial Activity of Nanomaterials
B. Rajak (2020)
Innovative coenzyme Q10-loaded nanoformulation as an adjunct approach for the management of moderate periodontitis: preparation, evaluation, and clinical study
Mohamed A. Shaheen (2020)
Second-generation antipsychotics and metabolism alterations: a systematic review of the role of the gut microbiome
K. Skonieczna-Żydecka (2018)
Do your gut microbes affect your brain dopamine?
Camila González-Arancibia (2019)
Chlorpromazine and Amitriptyline Are Substrates and Inhibitors of the AcrB Multidrug Efflux Pump
Elizabeth M Grimsey (2020)
Propranolol, chlorpromazine and diclofenac restore susceptibility of extensively drug-resistant (XDR)-Acinetobacter baumannii to fluoroquinolones
Mostafa A Mohammed (2020)
Psychotropics and the Microbiome: a Chamber of Secrets…
S. Cussotto (2019)
Carbohydrate-based Trojan microparticles as carriers for pulmonary delivery of lipid nanocapsules using dry powder inhalation
Anita Umerska (2020)
The role of the gut microbiome in the development of schizophrenia
J. Kelly (2020)
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