In vitro antibacterial activity and in vivo pharmacokinetics of intravenously administered Amikacin-loaded Liposomes for the management of bacterial septicaemia

Maxwell, Amala; Chaudhari, Bhim Bahadur; Chaudhari, Pinal; Koteshwara, Ananthamurthy; Aranjani, Jesil Mathew; Moorkoth, Sudheer; Ghate, Vivek; Lewis, Shaila

doi:10.1016/j.colsurfb.2022.112892

Cited by 2 publications

(1 citation statement)

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“…On the one hand, this may be accomplished by the discovery of new antibacterial drugs, a time- and cost-inefficient process. On the other hand, drug repurposing using nanotechnology has been accomplished mainly through the association of clinically approved antibiotics within delivery systems, namely liposomes [ 19 , 20 , 21 , 22 , 23 ]. Compared to the process of drug discovery and development, the repurposing of existing antibiotics entails shorter timelines and fewer costs [ 19 , 20 ].…”

Section: Introductionmentioning

confidence: 99%

Liposomal Rifabutin—A Promising Antibiotic Repurposing Strategy against Methicillin-Resistant Staphylococcus aureus Infections

Pinho,

Ferreira,

Coelho

et al. 2024

Pharmaceuticals

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Methicillin-resistant Staphylococcus aureus (M RSA) infections, in particular biofilm-organized bacteria, remain a clinical challenge and a serious health problem. Rifabutin (RFB), an antibiotic of the rifamycins class, has shown in previous work excellent anti-staphylococcal activity. Here, we proposed to load RFB in liposomes aiming to promote the accumulation of RFB at infected sites and consequently enhance the therapeutic potency. Two clinical isolates of MRSA, MRSA-C1 and MRSA-C2, were used to test the developed formulations, as well as the positive control, vancomycin (VCM). RFB in free and liposomal forms displayed high antibacterial activity, with similar potency between tested formulations. In MRSA-C1, minimal inhibitory concentrations (MIC) for Free RFB and liposomal RFB were 0.009 and 0.013 μg/mL, respectively. Minimum biofilm inhibitory concentrations able to inhibit 50% biofilm growth (MBIC50) for Free RFB and liposomal RFB against MRSA-C1 were 0.012 and 0.008 μg/mL, respectively. Confocal microscopy studies demonstrated the rapid internalization of unloaded and RFB-loaded liposomes in the bacterial biofilm matrix. In murine models of systemic MRSA-C1 infection, Balb/c mice were treated with RFB formulations and VCM at 20 and 40 mg/kg of body weight, respectively. The in vivo results demonstrated a significant reduction in bacterial burden and growth index in major organs of mice treated with RFB formulations, as compared to Control and VCM (positive control) groups. Furthermore, the VCM therapeutic dose was two fold higher than the one used for RFB formulations, reinforcing the therapeutic potency of the proposed strategy. In addition, RFB formulations were the only formulations associated with 100% survival. Globally, this study emphasizes the potential of RFB nanoformulations as an effective and safe approach against MRSA infections.

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