Abstract

Cyclic lipopeptides produced by Bacillus species exhibit interesting therapeutic potential. However, their clinical use remains limited due to their low stability, undesirable interactions with host macromolecules, and their potential toxicity to mammalian cells. The present work aims to develop suitable lipopeptide-loaded chitosan nanoparticles with improved biological properties and reduced toxicity. Surfactin and bacillomycin D lipopeptides produced by Bacillus amyloliquefaciens B84 strain were loaded onto chitosan nanoparticles by ionotropic gelation process. Nanoformulated lipopeptides exhibit an average size of 569nm, a zeta potential range of 38.8mV, and encapsulation efficiency (EE) of 85.58%. Treatment of Candida (C.) albicans cells with encapsulated lipopeptides induced anti-adhesive activity of 81.17% and decreased cell surface hydrophobicity (CSH) by 25.53% at 2000µg/mL. Nanoformulated lipopeptides also induced antileishmanial activity against Leishmania (L.) major promastigote and amastigote forms at respective IC50 values of 14.37µg/mL and 22.45µg/mL. Nanoencapsulated lipopeptides exerted low cytotoxicity towards human erythrocytes and Raw 264.7 macrophage cell line with respective HC50 and LC50 values of 770µg/mL and 234.56µg/mL. Nanoencapsulated lipopeptides could be used as a potential delivery system of lipopeptides to improve their anti-adhesive effect against C. albicans cells colonizing medical devices and their anti-infectious activity against leishmania.

Highlights

  • The pathogenic yeast Candida albicans has the ability to colonize surfaces including biomedical devices such as catheters and prostheses [1]

  • Data showed that strain B84 produced 68.83% surfactin homologues and 31.16% bacillomycin D homologues

  • The results showed that the LP was more active than the LP/chitosan nanoparticles (Cs-NPs) when tested against Candida cells with minimal inhibitory concentration (MIC) of 156 and 312 μg mL-1 respectively

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Summary

Introduction

The pathogenic yeast Candida albicans has the ability to colonize surfaces including biomedical devices such as catheters and prostheses [1]. This pathogen develops a biofilm which consists of a wellstructured surface cell community that is responsible for pathogenesis and plays an important role in the protection of cells against host defense and conventional antifungal drugs [2]. Lipopeptides affect the adhesion of microorganisms by modifying cell surface properties [8]. They have the capacity to adsorb to microbial surfaces, resulting in a change in the hydrophobicity of the cell surface and a decrease in the adhesion process [9]

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