Cationic compounds are promising candidates for development of antimicrobial agents. Positive charges attached to surfaces, particles, polymers, peptides or bilayers have been used as antimicrobial agents by themselves or in sophisticated formulations. The main positively charged moieties in these natural or synthetic structures are quaternary ammonium groups, resulting in quaternary ammonium compounds (QACs). The advantage of amphiphilic cationic polymers when compared to small amphiphilic molecules is their enhanced microbicidal activity. Besides, many of these polymeric structures also show low toxicity to human cells; a major requirement for biomedical applications. Determination of the specific elements in polymers, which affect their antimicrobial activity, has been previously difficult due to broad molecular weight distributions and random sequences characteristic of radical polymerization. With the advances in polymerization control, selection of well defined polymers and structures are allowing greater insight into their structure-antimicrobial activity relationship. On the other hand, antimicrobial polymers grafted or self-assembled to inert or non inert vehicles can yield hybrid antimicrobial nanostructures or films, which can act as antimicrobials by themselves or deliver bioactive molecules for a variety of applications, such as wound dressing, photodynamic antimicrobial therapy, food packing and preservation and antifouling applications.

BackgroundSeveral cationic polymers exhibit a useful antimicrobial property, however the structure–activity relationship still requires a more complete investigation. The main objective of this work is the comparison between the antimicrobial activity and toxicity of free and immobilized poly (diallyldimethylammonium) chloride (PDDA) in biocompatible poly (methylmethacrylate) (PMMA) nanoparticles (NPs).ResultsNPs synthesis by emulsion polymerization is performed over a range of [PDDA] at two methylmethacrylate (MMA) concentrations. The PMMA/PDDA dispersions are characterized by dynamic light-scattering for sizing, polydispersity and zeta-potential analysis, scanning electron microscopy (SEM), plating plus colony forming unities (CFU) counting for determination of the minimal microbicidal concentrations (MMC) against Escherichia coli, Staphylococcus aureus and Candida albicans and hemolysis evaluation against mammalian erythrocytes. There is a high colloidal stability for the cationic PMMA/PDDA NPs over a range of [PDDA]. NPs diverse antimicrobial activity against the microorganisms reduces cell viability by eight-logs (E. coli), seven-logs (S. aureus) or two-logs (C. albicans). The NPs completely kill E. coli over a range of [PDDA] that are innocuous to the erythrocytes. Free PDDA antimicrobial activity is higher than the one observed for PDDA in the NPs. There is no PDDA induced-hemolysis at the MMC in contrast to the hemolytic effect of immobilized PDDA in the NPs. Hemolysis is higher than 15 % for immobilized PDDA at the MMC for S. aureus and C. albicans.ConclusionsThe mobility of the cationic antimicrobial polymer PDDA determines its access to the inner layers of the cell wall and the cell membrane, the major sites of PDDA antimicrobial action. PDDA freedom does matter for determining the antimicrobial activity at low PDDA concentrations and absence of hemolysis.Electronic supplementary materialThe online version of this article (doi:10.1186/s12951-015-0123-3) contains supplementary material, which is available to authorized users.

Peptides in general hold much promise as a major ingredient in novel supramolecular assemblies. They may become essential in vaccine design, antimicrobial chemotherapy, cancer immunotherapy, food preservation, organs transplants, design of novel materials for dentistry, formulations against diabetes and other important strategical applications. This review discusses how novel formulations may improve the therapeutic index of antimicrobial peptides by protecting their activity and improving their bioavailability. The diversity of novel formulations using lipids, liposomes, nanoparticles, polymers, micelles, etc., within the limits of nanotechnology may also provide novel applications going beyond antimicrobial chemotherapy.

The purpose of this Article is to characterize polymeric particles of poly(methylmethacrylate) (PMMA) synthesized in the presence of one of two different quaternary ammonium surfactants (QACs): cetyltrimethylammonium bromide (CTAB) or dioctadecyldimethylammonium bromide (DODAB). The methods used are dynamic light scattering for sizing, polydispersity and zeta potential analysis, scanning electron microscopy (SEM) for morphology visualization, and plating plus colony-forming unities (CFU) counting for the determination of antimicrobial activity. The results point out the high QAC concentration required to obtain cationic and bioactive antimicrobial particles with good colloidal stability and a permanent load of the polymeric network with QACs. Over a range of micromolar QAC concentrations, there is remarkable antimicrobial activity of PMMA/CTAB or PMMA/DODAB particles, which is much higher than those determined for the QACs by themselves. Loading the biocompatible polyacrylate particles with QACs is a facile, fast, low-cost approach to obtaining highly efficient antimicrobial nanoparticles.

The growing challenge of antimicrobial resistance to antibiotics requires novel synthetic drugs or new formulations for old drugs. Here, cationic nanostructured particles (NPs) self-assembled from cationic bilayer fragments and polyelectrolytes are tested against four multidrug-resistant (MDR) strains of clinical importance. The non-hemolytic poly(diallyldimethylammonium) chloride (PDDA) polymer as the outer NP layer shows a remarkable activity against these organisms. The mechanism of cell death involves bacterial membrane lysis as determined from the leakage of inner phosphorylated compounds and possibly disassembly of the NP with the appearance of multilayered fibers made of the NP components and the biopolymers withdrawn from the cell wall. The NPs display broad-spectrum activity against MDR microorganisms, including Gram-negative and Gram-positive bacteria and yeast.