Abstract

Their stability and low cost make catanionic vesicles suitable for application as drug delivery systems. In this work we prepared catanionic vesicles using biocompatible surfactants: two cationic arginine-based surfactants (the monocatenary Nα-lauroyl-arginine methyl ester—LAM and the gemini Nα,Nϖ-bis(Nα-lauroylarginine) α, ϖ-propylendiamide—C3(CA)2) and three anionic amphiphiles (the single chain sodium dodecanoate, sodium myristate, and the double chain 8-SH). The critical aggregation concentration, colloidal stability, size, and charge density of these systems were comprehensively studied for the first time. These catanionic vesicles, which form spontaneously after mixing two aqueous solutions of oppositely charged surfactants, exhibited a monodisperse population of medium-size aggregates and good stability. The antimicrobial and hemolytic activity of the vesicles can be modulated by changing the cationic/anionic surfactant ratio. Vesicles with a positive charge efficiently killed Gram-negative and Gram-positive bacteria as well as yeasts; the antibacterial activity declined with the decrease of the cationic charge density. The catanionic systems also effectively eradicated MRSA (Methicillin-resistant Staphylococcus Aureus) and Pseudomonas aeruginosa biofilms. Interestingly, the incorporation of cholesterol in the catanionic mixtures improved the stability of these colloidal systems and considerably reduced their cytotoxicity without affecting their antimicrobial activity. Additionally, these catanionic vesicles showed good DNA affinity. Their antimicrobial efficiency and low hemolytic activity render these catanionic vesicles very promising candidates for biomedical applications.

Highlights

  • The versatile vesicular nanosystems have attracted considerable attention due to their promising therapeutic applications

  • The size distribution of all formulations was determined by using the dynamic light scattering technique (DLS)

  • A single phase of catanionic vesicles is formed in the diluted cation- or anion-rich region of the surfactant [28]

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Summary

Introduction

The versatile vesicular nanosystems have attracted considerable attention due to their promising therapeutic applications. Catanionic vesicles [8], which spontaneously self-assemble without any energy requirements after the mixing of inexpensive cationic and anionic surfactant solutions [9], have been investigated as potential alternatives to liposomes Among their advantages, catanionic vesicles can be thermodynamically or kinetically stable for long periods of time, they can be prepared using simple and economic surfactants, and their size, surface density, flexibility, and permeability can be tailored by adjusting the concentration, cationic/anionic mixing ratio, temperature, and chain length of the components and the addition of salts or co-solvents [8]. The study had three main aims: first, to prepare catanionic mixtures using green biocompatible surfactants, second, to design new formulations with high antimicrobial activities and moderate toxicity and third, to shed light on how the mixing ratio, the number of alkyl chains in the ion pairs and the nature of polar heads affect the biological and physico-chemical properties of catanionic vesicles. We expect that the findings described in this work will contribute to the understanding of the biological activity of catanionic mixtures from amino acid-based surfactants and help to rationalize the design of new and safe antimicrobial formulations

Materials
Preparations of Catanionic Mixtures
Fluorescence Measurements
Conductivity
NMR Measurements
Antimicrobial Activity
Antibiofilm Activity
Hemolysis Assay
2.10. Ethidium Bromide Fluorescence
Critical Aggregation Concentration
Antibioffiilm Activity
Hemolytic Activity
DNA Binding Properties
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