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Medical Sciences Forum
  • Abstract
  • Open Access

1 November 2022

Resveratrol-Loaded Glycosylated Liposomes for Targeting Bacteria †

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1
Institute for Biological Systems, Italian National Research Council (ISB-CNR) Secondary Office of Rome-Reaction Mechanisms c/o Department of Chemistry, Sapienza University, P.le A. Moro 5, 00185 Rome, Italy
2
Department of Chemistry, Sapienza University, P.le A. Moro 5, 00185 Rome, Italy
3
Institute of Chemical Engineering Sciences (ICE-HT), Foundation for Research and Technology, Hellas (FORTH), Platani, 26504 Patras, Greece
4
Institute of Complex Systems, Italian National Research Council (ISC-CNR), Sede Sapienza c/o Physics Department, Sapienza University, P.le A. Moro 5, 00185 Rome, Italy
This article belongs to the Proceedings The 8th International Electronic Conference on Medicinal Chemistry
Biofilm-associated bacterial diseases are a major health problem due to the high antibiotic resistance of biofilm infections [1,2]. In recent years, several methods, some of which rely on nanotechnology [3], have been developed to tackle this problem. The search for non-antibiotic strategies has renewed interest in natural molecules that exploit alternative bacterial-fighting mechanisms and, above all, do not induce resistance. In this context, we have developed two sets of cationic glycosylated liposomes for the targeted delivery of trans-resveratrol (RSV), a secondary plant metabolite with antimicrobial properties, to bacteria that express carbohydrate-specific proteins able to recognize monosaccharides, namely Staphylococcus epidermidis [4] and Methicillin Resistant Staphylococcus Aureus (MRSA) [5]. Liposome physico-chemical properties (diameter, polidispersity index-PDI-, charge, and RSV entrapment efficiency) were measured by dynamic light scattering (DLS), electrophoretic mobility, and high-performance liquid chromatography (HPLC). Liposomes used in the experiments on MRSA were composed of 1,2-dioleoyl-sn-glycero-3-phosphocholine, cholesterol (Chol), and glycoamphiphiles featuring a galactosyl, mannosyl, or glucosyl moiety [5]. The objective was to identify the best sugar moiety to target MRSA biofilm. Microbiological tests carried out to monitor the demolition effect of RSV-loaded liposomes on MRSA mature biofilms showed that RSV-galactosylated liposomes are the most effective at an RSV concentration 60 times below the minimum inhibitory concentration (MIC). Liposomes used in the experiments on S. epidermidis were formulated with 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, Chol, and the glycoamphiphile featuring the glucose residue [4]. The ability of RSV-loaded liposomes to inhibit the growth of a slime-positive and a slime-negative strain of S. epidermidis was evaluated. Glucosylated liposomes, which are non-toxic, kill bacteria at concentrations tenfold under the MIC of RSV.

Supplementary Materials

The following are available online at https://www.mdpi.com/article/10.3390/ECMC2022-13158/s1.

Author Contributions

C.B.: Conceptualization, Methodology, Project administration, Writing—original draft, Visualization, Writing—review & editing; L.P.: Investigation, Visualization; S.A.: Investigation, Visualization; F.G.: Investigation, Visualization; B.S.: Investigation, Visualization; F.C.: Validation, Visualization, Writing—review & editing; S.S.: Investigation, Formal analysis; A.C.: Methodology, Investigation; F.B.: Methodology, Validation, Writing—review & editing, Supervision; C.M.: Investigation; M.S.: Supervision; R.T.: Investigation, Formal analysis, Visualization; S.M.: Methodology, Investigation; I.S.: Methodology, Supervision. S.G.A.: Supervision, Validation; G.M.: Conceptualization, Supervision. All authors have read and agreed to the published version of the manuscript.

Funding

This research received no external funding.

Data Availability Statement

Data supporting the presented data are published in [4,5].

Conflicts of Interest

The authors declare no conflict of interest.

References

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