Abstract

Currently, one of the greatest health challenges worldwide is the resistance to antibiotic drugs, which has led to the pursuit of new alternatives for the recovery of biological activity, where the use of different types of nano-systems has shown an interesting potential. In this study, we evaluated the antibiotic activity of a model drug (ampicillin) encapsulated within coated-nanoliposomes on strains of Staphylococcus aureus with different antibiotic-resistance degrees. Hence, liposomes were elaborated by the ethanol injection method and were coated with a cationic polymer (Eudragit E-100) through the layer-by-layer process. Liposome characterization, such as size, polydispersity, zeta potential, and encapsulation efficiency were determined using dynamic light scattering and ultrafiltration/centrifugation techniques. Although biological activity was evaluated using three ATCC strains of S. aureus corresponding to ATCC 25923 (sensitive), ATCC 29213 (resistant) and ATCC 43300 (very resistant). The results showed changes in size (from ~150 to 220 nm), polydispersity (from 0.20 to 0.45) and zeta potential (from −37 to +45 mV) for the coating process. In contrast, encapsulation efficiency of approximately 70% and an increase in antibiotic activity of 4 and 18 times more on those S. aureus-resistant strains have been observed.

Highlights

  • Antimicrobial resistance has been considered one of the greatest challenges in medicine according to the World Health Organization because this problem leads to the conventional therapy for many infectious diseases becoming difficult to treat [1]

  • With the aim of contributing to finding solutions to this complex problem, we have been working in our laboratory regarding the use of nanoparticle technology as a potential strategy to help recover the biological activity of antibiotic drugs with resistance problems

  • It could be expected that agglomeration of the phospholipids will be greater at the interface for longer aging times; vesicles will form with a larger size

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Summary

Introduction

Antimicrobial resistance has been considered one of the greatest challenges in medicine according to the World Health Organization because this problem leads to the conventional therapy for many infectious diseases becoming difficult to treat [1]. There is a great diversity of microorganisms associated with this problem, Staphylococcus aureus has been highlighted to be one of the most relevant due to its high recurrence, making it one of the primary pathogens with resistance problems worldwide [6] Such microorganism has generated several specific mechanisms of resistance, where the production of specialized enzymes (β-lactamases) is one of the most used complexes because it has inactivated many conventional β-lactam antibiotic drugs [7]. Liposomes have shown very interesting results due to their biocompatibility features, ease of processing, and versatility in modifying and conferring new properties [19,20] In this regard, liposomes coated with polymers have been called in different ways, such as ‘colloidosomes’ or ‘stealth liposomes’ when ionic polymers or polymer derivative of polyethylene-glycol is used, respectively, which could be an interesting alternative in overcoming drug-resistance problems [1,21,22,23]. Several types of polymer–drug nanocomplexes have been evaluated on

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