Enhancing azithromycin antibacterial activity by encapsulation in liposomes/liposomal-N-acetylcysteine formulations against resistant clinical strains of Escherichia coli

Aljihani, Shokran A.; Alehaideb, Zeyad; Alarfaj, R; Alghoribi, Majed F.; Akiel, Maaged; Alenazi, Thamer H.; Alfahad, Ahmed J.; Tamimi, Saad M. Al; Albakr, Turki M.; Alshehri, Abdulrahman; Alyahya, Saad M.; Yassin, Alaa Eldeen B.; Halwani, Majed

doi:10.1016/j.sjbs.2020.09.012

Cited by 16 publications

(9 citation statements)

References 22 publications

(30 reference statements)

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“…Analyzing the MIC of the different formulations showed that the AZM-ZnONP formulation was very effective against both MRSA and E. coli and the MIC was reduced markedly compared to each of them when used alone. Similarly, Aljihani, et al [48] reported that liposomal AZM and liposomal AZM/N-acetyl cysteine markedly improved the MIC of AZM against E. coli. Another study showed that AZM nanoparticles produced the same inhibitory effect against E. coli at an eight times lower concentration compared to free AZM [70].…”

Section: In Vitro and In Vivo Antibacterial Activitiesmentioning

confidence: 87%

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Tailoring of Novel Azithromycin-Loaded Zinc Oxide Nanoparticles for Wound Healing

et al. 2022

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Skin is the largest mechanical barrier against invading pathogens. Following skin injury, the healing process immediately starts to regenerate the damaged tissues and to avoid complications that usually include colonization by pathogenic bacteria, leading to fever and sepsis, which further impairs and complicates the healing process. So, there is an urgent need to develop a novel pharmaceutical material that promotes the healing of infected wounds. The present work aimed to prepare and evaluate the efficacy of novel azithromycin-loaded zinc oxide nanoparticles (AZM-ZnONPs) in the treatment of infected wounds. The Box–Behnken design and response surface methodology were used to evaluate loading efficiency and release characteristics of the prepared NPs. The minimum inhibitory concentration (MIC) of the formulations was determined against Staphylococcus aureus and Escherichia coli. Moreover, the anti-bacterial and wound-healing activities of the AZM-loaded ZnONPs impregnated into hydroxyl propyl methylcellulose (HPMC) gel were evaluated in an excisional wound model in rats. The prepared ZnONPs were loaded with AZM by adsorption. The prepared ZnONPs were fully characterized by XRD, EDAX, SEM, TEM, and FT-IR analysis. Particle size distribution for the prepared ZnO and AZM-ZnONPs were determined and found to be 34 and 39 nm, respectively. The mechanism by which AZM adsorbed on the surface of ZnONPs was the best fit by the Freundlich model with a maximum load capacity of 160.4 mg/g. Anti-microbial studies showed that AZM-ZnONPs were more effective than other controls. Using an experimental infection model in rats, AZM-ZnONPs impregnated into HPMC gel enhanced bacterial clearance and epidermal regeneration, and stimulated tissue formation. In conclusion, AZM -loaded ZnONPs are a promising platform for effective and rapid healing of infected wounds.

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Section: In Vitro and In Vivo Antibacterial Activitiesmentioning

confidence: 87%

“…The MICs of the AZM, ZnO, and AZM-loaded ZnONPs were determined against the clinical MRSA and E. coli isolates using the broth dilution technique [48]. Firstly, different formulations were serially diluted in a 96-well plate in Mueller-Hinton broth starting at a concentration of 200 µg/mL.…”

Section: Determination Of the Minimal Inhibitory Concentration (Mic)mentioning

confidence: 99%

Tailoring of Novel Azithromycin-Loaded Zinc Oxide Nanoparticles for Wound Healing

et al. 2022

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“…RUT starts to lose its weight from 45 °C, but when it was formulated as liposomes, degradation starts at 225 °C, which ensures the stability of RUT in the liposomal vesicle. Stability of other excipients such as HSPC, TPGS, and cholesterol was also observed to be improved as before formulating they were showing a sharp decline in weight loss, but when it was formulated as RUT-LIPO, the weight loss was observed in a progressive manner at a wide range of temperatures (Figure C) …”

Section: Discussionmentioning

confidence: 92%

GPIIb/IIIa Receptor Targeted Rutin Loaded Liposomes for Site-Specific Antithrombotic Effect

et al. 2022

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Rutin (RUT) is a flavonoid obtained from a natural source and is reported for antithrombotic potential, but its delivery remains challenging because of its poor solubility and bioavailability. In this research, we have fabricated novel rutin loaded liposomes (RUT-LIPO, nontargeted), liposomes conjugated with RGD peptide (RGD-RUT-LIPO, targeted), and abciximab (ABX-RUT-LIPO, targeted) by ethanol injection method. The particle size, ζ potential, and morphology of prepared liposomes were analyzed by using DLS, SEM, and TEM techniques. The conjugation of targeting moiety on the surface of targeted liposomes was confirmed by XPS analysis and Bradford assay. In vitro assessment such as blood clot assay, aPTT assay, PT assay, and platelet aggregation analysis was performed using human blood which showed the superior antithrombotic potential of ABX-RUT-LIPO and RGD-RUT-LIPO liposomes. The clot targeting efficiency was evaluated by in vitro imaging and confocal laser scanning microscopy. A significant (P < 0.05) rise in the affinity of targeted liposomes toward activated platelets was demonstrated that revealed their remarkable potential in inhibiting thrombus formation. Furthermore, an in vivo study executed on Sprague Dawley rats (FeCl3 model) demonstrated improved antithrombotic activity of RGD-RUT-LIPO and ABX-RUT-LIPO compared with pure drug. The pharmacokinetic study performed on rats demonstrates the increase in bioavailability when administered as liposomal formulation as compared to RUT. Moreover, the tail bleeding assay and clotting time study (Swiss Albino mice) indicated a better antithrombotic efficacy of targeted liposomes than control preparations. Additionally, biocompatibility of liposomal formulations was determined by an in vitro hemolysis study and cytotoxicity assay, which showed that they were hemocompatible and safe for human use. A histopathology study on rats suggested no severe toxicity of prepared liposomal formulations. Thus, RUT encapsulated nontargeted and targeted liposomes exhibited superior antithrombotic potential over RUT and could be used as a promising carrier for future use.

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“… 130 A liposomal formulation of co-encapsulated azithromycin and N-acetylcysteine has been demonstrated to have a synergistic effect against bacterial strains. 131 The high cellular membrane permeability and targeting accuracy associated with such a delivery system illuminates a potential implication for the co-formulation strategy of N-acetylcysteine with antiviral drug.…”

Section: Discussionmentioning

confidence: 99%

N-Acetylcysteine as Adjuvant Therapy for COVID-19 – A Perspective on the Current State of the Evidence

Wong¹,

Lee²,

Kua³

2021

JIR

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The looming severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has caused a long-lasting pandemic of coronavirus disease 2019 around the globe with substantial morbidity and mortality. N-acetylcysteine, being a nutraceutical precursor of an important antioxidant glutathione, can perform several biological functions in mammals and microbes. It has consequently garnered a growing interest as a potential adjunctive therapy for coronavirus disease. Here, we review evidence concerning the effects of N-acetylcysteine in respiratory viral infections based on currently available in vitro, in vivo, and human clinical investigations. The repurposing of a known drug such as N-acetylcysteine may significantly hasten the deployment of a novel approach for COVID-19. Since the drug candidate has already been translated into the clinic for several decades, its established pharmacological properties and safety and side-effect profiles expedite preclinical and clinical assessment for the treatment of COVID-19. In vitro data have depicted that N-acetylcysteine increases antioxidant capacity, interferes with virus replication, and suppresses expression of pro-inflammatory cytokines in cells infected with influenza viruses or respiratory syncytial virus. Furthermore, findings from in vivo studies have displayed that, by virtue of immune modulation and anti-inflammatory mechanism, N-acetylcysteine reduces the mortality rate in influenza-infected mice animal models. The promising in vitro and in vivo results have prompted the initiation of human subject research for the treatment of COVID-19, including severe pneumonia and acute respiratory distress syndrome. Albeit some evidence of benefits has been observed in clinical outcomes of patients, precision nanoparticle design of N-acetylcysteine may allow for greater therapeutic efficacy.

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Enhancing azithromycin antibacterial activity by encapsulation in liposomes/liposomal-N-acetylcysteine formulations against resistant clinical strains of Escherichia coli

Cited by 16 publications

References 22 publications

Tailoring of Novel Azithromycin-Loaded Zinc Oxide Nanoparticles for Wound Healing

Tailoring of Novel Azithromycin-Loaded Zinc Oxide Nanoparticles for Wound Healing

GPIIb/IIIa Receptor Targeted Rutin Loaded Liposomes for Site-Specific Antithrombotic Effect

N-Acetylcysteine as Adjuvant Therapy for COVID-19 – A Perspective on the Current State of the Evidence

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