Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Daptomycin Liposomes Exhibit Enhanced Activity against Staphylococci Biofilms Compared to Free Drug

Foteini Gkartziou
* ,
Maria Plota
ORCID logo ,
Charikleia Kypraiou
,
Iti Gauttam
,
Kolonitsiou Fevronia
ORCID logo ,
Pavlos Klepetsanis
,
Iris Spiliopoulou
,
Sophia G Antimisiaris
* ORCID logo
Version 1 : Received: 24 February 2024 / Approved: 26 February 2024 / Online: 26 February 2024 (12:00:24 CET)

A peer-reviewed article of this Preprint also exists.

Gkartziou, F.; Plota, M.; Kypraiou, C.; Gauttam, I.; Kolonitsiou, F.; Klepetsanis, P.; Spiliopoulou, I.; Antimisiaris, S.G. Daptomycin Liposomes Exhibit Enhanced Activity against Staphylococci Biofilms Compared to Free Drug. Pharmaceutics 2024, 16, 459. Gkartziou, F.; Plota, M.; Kypraiou, C.; Gauttam, I.; Kolonitsiou, F.; Klepetsanis, P.; Spiliopoulou, I.; Antimisiaris, S.G. Daptomycin Liposomes Exhibit Enhanced Activity against Staphylococci Biofilms Compared to Free Drug. Pharmaceutics 2024, 16, 459.

Abstract

The purpose of the present study was to investigate anti-staphylococcal activity of liposomal daptomycin, against four biofilm-producing S. aureus and S. epidermidis clinical strains, three of which are methicillin resistant. Neutral and negatively charged Daptomycin-loaded liposomes were prepared by three methods thin film hydration (TFH), DRV and microfluidic mixing (MM), and characterized for drug encapsulation (EE%), size distribution, zeta-potential, vesicle stability, drug release and drug integrity. Interestingly, whilst drug loading in THF and DRV nanosized (by extrusion) vesicles was around 30-35, very low loading (~4%) was possible in MM vesicles, requiring further explanatory investigations. Liposomal encapsulation protected daptomycin from degradation and preserve its bioactivity. Quantitative microtiter plate (crystal violet, CV), methylthiazoltetrazolium (MTT), and growth curve (GC) assays evaluated antimicrobial activity of neutral and negative charge daptomycin-liposomes towards planktonic bacteria and biofilms. Neutral liposomes exhibited dramatically enhanced inhibition of bacteria growth (compared to free drug) for all species studied, while negative charged liposomes were totally inactive. Biofilm prevention and treatment studies revealed high antibiofilm activity of liposomal daptomycin. Neutral liposomes were more active for prevention and negative charge ones for treating established biofilms. Planktonic bacteria as well as matured biofilms of low daptomycin susceptible MRSE and MRSA strains were almost completely eradicated by liposomal-daptomycin indicating the need for their further exploration as antimicrobial therapeutics.

Keywords

Daptomycin; liposomes; zeta-potential; bacteriostatic; biofilm; growth inhibition; MRSA; MRSE; Integrity

Subject

Medicine and Pharmacology, Other

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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