Effect of Polyhexamethylene Biguanide in Combination with Undecylenamidopropyl Betaine or PslG on Biofilm Clearance

Hospital-acquired infection is a great challenge for clinical treatment due to pathogens’ biofilm formation and their antibiotic resistance. Here, we investigate the effect of antiseptic agent polyhexamethylene biguanide (PHMB) and undecylenamidopropyl betaine (UB) against biofilms of four pathogens that are often found in hospitals, including Gram-negative bacteria Pseudomonas aeruginosa and Escherichia coli, Gram-positive bacteria Staphylococcus aureus, and pathogenic fungus, Candida albicans. We show that 0.02% PHMB, which is 10-fold lower than the concentration of commercial products, has a strong inhibitory effect on the growth, initial attachment, and biofilm formation of all tested pathogens. PHMB can also disrupt the preformed biofilms of these pathogens. In contrast, 0.1% UB exhibits a mild inhibitory effect on biofilm formation of the four pathogens. This concentration inhibits the growth of S. aureus and C. albicans yet has no growth effect on P. aeruginosa or E. coli. UB only slightly enhances the anti-biofilm efficacy of PHMB on P. aeruginosa biofilms. However, pretreatment with PslG, a glycosyl hydrolase that can efficiently inhibit and disrupt P. aeruginosa biofilm, highly enhances the clearance effect of PHMB on P. aeruginosa biofilms. Meanwhile, PslG can also disassemble the preformed biofilms of the other three pathogens within 30 min to a similar extent as UB treatment for 24 h.     

Polyphenylglyoxamide-Based Amphiphilic Small Molecular Peptidomimetics as Antibacterial Agents with Anti-Biofilm Activity

The rapid emergence of drug-resistant bacteria is a major global health concern. Antimicrobial peptides (AMPs) and peptidomimetics have arisen as a new class of antibacterial agents in recent years in an attempt to overcome antibiotic resistance. A library of phenylglyoxamide-based small molecular peptidomimetics was synthesised by incorporating an N-alkylsulfonyl hydrophobic group with varying alkyl chain lengths and a hydrophilic cationic group into a glyoxamide core appended to phenyl ring systems. The quaternary ammonium iodide salts 16d and 17c showed excellent minimum inhibitory concentration (MIC) of 4 and 8 μM (2.9 and 5.6 μg/mL) against Staphylococcus aureus, respectively, while the guanidinium hydrochloride salt 34a showed an MIC of 16 μM (8.5 μg/mL) against Escherichia coli. Additionally, the quaternary ammonium iodide salt 17c inhibited 70% S. aureus biofilm formation at 16 μM. It also disrupted 44% of pre-established S. aureus biofilms at 32 μM and 28% of pre-established E. coli biofilms 64 μM, respectively. A cytoplasmic membrane permeability study indicated that the synthesised peptidomimetics acted via disruption and depolarisation of membranes. Moreover, the quaternary ammonium iodide salts 16d and 17c were non-toxic against human cells at their therapeutic dosages against S. aureus.     

Evaluation of antithrombogenic and antibacterial activities of a graphite oxide/heparin-benzalkonium chloride composite

A graphite oxide (GO)/heparin-benzalkonium chloride (C12) composite was synthesized. The composite was characterized by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). XRD data showed that spacing between layers of GO increased from 0.59 to 3.256 nm. This enlarged layer spacing suggested that heparin-C12 complex intercalated completely in between layers of GO. FTIR also confirmed intercalation of heparin-C12 complex into GO gallery. In vitro release rate of heparin from GO-heparin-C12 was monitored for 30 days. Heparin released at a very fast rate from the composite matrix in the first day. The release slowed down significantly after the first day and continued for 30 days. In addition, antibacterial activity of the composite against Escherichia coli (E. coli) and Staphlococcus aureus (S. aureus) was evaluated using zone of inhibition and colony count assays. Both GO-heparin-C12 and GO-C12 clearly showed antibacterial activity against E. coli and S. aureus while GO alone has a relatively low activity against S. aureus and almost no effect on E. coli.     

<Emphasis Type="SmallCaps">d</Emphasis>-Maltose Synthesized Silver Nanoparticles for Biofilm Eradication

Biofilms are complex bacterial communities have a mechanism for antibiotic resistance leading to human health problems. It remains challenging to treat and eradicate biofilms. In this work, the use of d-maltose synthesized silver nanoparticles (AgNPs) was investigated in an effort to eradicate a biofilm. AgNPs were synthesized using a modified Tollen’s method. d-maltose was used in synthesizing AgNPs with different concentrations of d-maltose (0.01, 0.05 and 0.1 M), referred to as NP1, NP2 and NP3, respectively. TEM images revealed that the particles were polygon shaped. The particle sizes were found to be 86.81?±?13.39, 54.94?±?11.63 and 31.43?±?31.76 nm depending on their sugar concentrations. UV–Vis, ATR–FTIR, and XRD patterns were employed to characterize the AgNPs. Then, these AgNPs were investigated for their anti-bacterial effects against Escherichia coli and Staphylococcus aureus. Evaluation of the minimum inhibitory concentration and minimal bactericidal concentration revealed that S. aureus was inhibited by all AgNPs and killed by NP1 and NP3, and E. coli was inhibited and killed at all AgNPs doses. Furthermore, anti-biofilm activity against these two bacteria was observed using SEM and confocal laser scanning microscopy. This sugar coated AgNPs is a promising material for use in eradication of biofilms.     

Enhanced the dispersibility and permeability of silver nanoparticles over rGO grafted by positively-charged polyethyleneimine toward broad-spectrum sterilization

Silver nanoparticles (Ag NPs) are used as antimicrobial agents due to their high-efficiency, broad-spectrum disinfection activity. However, the agglomeration and stability problems caused by excessive release of silver ions (Ag⁺) have severely restricted their developments. Herein, a novel silver/polyethyleneimine/reduced graphene oxide (Ag/PEI/rGO) antibacterial material featuring good dispersibility and permeability was rationally designed, thus benefiting for the capture of bacteria due to the introducing of highly-cationic PEI modifier and controllable release of biocidal agents (Ag⁺). Compared with Ag/rGO, the Ag/PEI/rGO has excellent stability and shows a more efficient sterilization efficacy against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) with 100% germicidal efficiency with low orders of dozens of ppm. In addition, the outstanding biocompatibility of this Ag/PEI/rGO antibacterial material endows it with promising potential in sterilization applications, which is expected to solve the infection problem caused by bacterial biofilm formation.     

The Antimicrobial Peptide Temporin G: Anti-Biofilm,Anti-Persister Activities,and Potentiator Effect of Tobramycin Efficacy Against Staphylococcus aureus

Bacterial biofilms are a serious threat for human health, and the Gram-positive bacterium Staphylococcus aureus is one of the microorganisms that can easily switch from a planktonic to a sessile lifestyle, providing protection from a large variety of adverse environmental conditions. Dormant non-dividing cells with low metabolic activity, named persisters, are tolerant to antibiotic treatment and are the principal cause of recalcitrant and resistant infections, including skin infections. Antimicrobial peptides (AMPs) hold promise as new anti-infective agents to treat such infections. Here for the first time, we investigated the activity of the frog-skin AMP temporin G (TG) against preformed S. aureus biofilm including persisters, as well as its efficacy in combination with tobramycin, in inhibiting S. aureus growth. TG was found to provoke ~50 to 100% reduction of biofilm viability in the concentration range from 12.5 to 100 µM vs ATCC and clinical isolates and to be active against persister cells (about 70–80% killing at 50–100 µM). Notably, sub-inhibitory concentrations of TG in combination with tobramycin were able to significantly reduce S. aureus growth, potentiating the antibiotic power. No critical cytotoxicity was detected when TG was tested in vitro up to 100 µM against human keratinocytes, confirming its safety profile for the development of a new potential anti-infective drug, especially for treatment of bacterial skin infections.     

2-(2-Methyl-2-nitrovinyl)furan but Not Furvina Interfere with Staphylococcus aureus Agr Quorum-Sensing System and Potentiate the Action of Fusidic Acid against Biofilms

Quorum sensing (QS) plays an essential role in the production of virulence factors, in biofilm formation and antimicrobial resistance. Consequently, inhibiting QS is being considered a promising target for antipathogenic/anti-virulence therapies. This study aims to screen 2-nitrovinylfuran derivatives structurally related to Furvina (a broad-spectrum antibiotic already used for therapeutic purposes) for their effects on QS and in biofilm prevention/control. Furvina and four 2-nitrovinylfuran derivatives (compounds 1–4) were tested to assess the ability to interfere with QS of Staphylococcus aureus using bioreporter strains (S. aureus ALC1742 and ALC1743). The activity of Furvina and the most promising quorum-sensing inhibitor (QSI) was evaluated in biofilm prevention and in biofilm control (combined with fusidic acid). The biofilms were further characterized in terms of biofilm mass, viability and membrane integrity. Compound 2 caused the most significant QS inhibition with reductions between 60% and 80%. Molecular docking simulations indicate that this compound interacts preferentially with the protein hydrophobic cleft in the LytTR domain of AgrA pocket. Metabolic inactivations of 40% for S. aureus ALC1742 and 20% for S. aureus ALC1743 were reached. A 24 h-old biofilm formed in the presence of the QSI increased the metabolic inactivation by fusidic acid to 80%, for both strains. The overall results highlight the effects of compound 2 as well as the potential of combining QSI with in-use antibiotics for the management of skin and soft tissues infections.     

PVA/PMMA polymer blended composite electrospun nanofibers mat and their potential use as an anti-biofilm product

Bacterial infections have increased dramatically due to microbial biofilm formation resulting in chronic pathological conditions in human subjects. Microbial biofilm causes poor drug penetration and antibiotic resistance, which has made site-specific sustained drug delivery the most appropriate option. Our work entails fabrication of ciprofloxacin hydrochloride (CPX) loaded nanofibers using polyvinyl alcohol (PVA) and poly(meth) methacrylate (PMMA) employing electrospinning method to form PVA:PMMA:CPX nanofibers mat. These nanofibers mat were optimized, characterized, and further subjected to anti-biofilm activity. Microscopic images revealed average nanofibers diameter of 243 ± 80 nm with smooth surface morphology. Analytical graphs and thermal analysis confirmed drug encapsulation and drug-polymer compatibility. In vitro studies demonstrated sustained release of CPX for 22 days displaying Hixon Crowell and two-stage desorption kinetics. Anti-biofilm activity showed zones of inhibition 3.0 ± 0.5 cm, 2.8 ± 0.1 cm, 2.9 ± 0.2 cm for Escherichia coli, Staphylococcus aureus, Enterococcus faecalis, respectively which was well above the minimum inhibitory concentration levels of the bacteria forming biofilm. Conclusively, these nanofibers mat have potential to be used as an anti-biofilm product.     

Drug loaded electrospun polymer/ceramic composite nanofibrous coatings on titanium for implant related infections

Developing an effective antibacterial surface with the help of drugs that prevent bacterial adhesion, colonization, and proliferation into the surrounding tissues is of great demand. Rifampicin (Rf) is effective antibiotic drug proved has proved its potential in treating bacteria in biofilms, especially against the microbes causing bone infections. Hydroxyapatite (HA), a biocompatible osteoconductive ceramic, has been verified to be a significant material for bioactivity enhancement. Electrospinning is an effective inexpensive method for incorporating nanoparticles into nanofibers with uniform distribution for the drug delivery system for tissue engineering applications. In the current study, for improving bioactivity and antibacterial properties, novel functional polycaprolactone (PCL) composite nanofibers loaded HA and Rf was developed and coated on titanium (Ti). Different characterization techniques such as SEM, EDS, XRD, FITR were used to analyze these PCL/Rf/HA nanocomposites. The results showed that the bioactivity and tensile strength of the composite scaffold increased with the addition of HA nanoparticles. In vitro bioactivity demonstrated that the PCL/HA/Rf composite nanofibers possess enhanced calcium deposition when compared to the pure sample. Cellular interactive responses such as adhesive and proliferation were evaluated using hFOB human fetal osteoblast cell lines. After 6 days of culturing, the cellular properties on Ti sample coated with PCL/HA/Rf was significantly improved. Antibacterial evaluations on the substrates showed that Rf-loaded PCL/HA fibers displayed >3 log reduction against S.aureus MRSA, and S.epidermidis bacterial strain and >2 log reduction against P.aeruginosa bacteria. In vitro drug release study shows initial burst release of Rf, followed by sustained released of 62% at the end of 32 days. The cell viability, adhesion, and proliferation evaluation suggest that the PCL/HA/Rf coated substrate possess good cytocompatibility. Further incorporation of Rf enhanced the antibacterial property of this nanofibrous scaffold.     

Antimicrobial activity of menthol modified nanodiamond particles

Advances in nanotechnology have seen the development of several microbiocidal nanoparticles displaying activity against biofilms. These applications benefit from one or more combinations of the nanoparticle properties. Nanoparticles may indeed concentrate drugs on their surface resulting in polyvalent effects and improved efficacy to fight against bacteria. Nanodiamonds (NDs) are among the most promising new materials for biomedical applications. We elucidate in this paper the effect of menthol modified nanodiamond (ND-menthol) particles on bacterial viability against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria. We show that while ND-menthol particles are non-toxic to both pathogens, they show significant antibiofilm activity. The presence of ND-menthol particles reduces biofilm formation more efficiently than free menthol, unmodified oxidized NDs and ampicillin, a commonly used antibiotic. Our findings might be thus a step forward towards the development of alternative non antibiotic based strategies targeting bacterial infections.     

Facile preparation and good performance of nano-Ag/metallocene polyethylene antibacterial coatings

Metallocene polyethylene/nano-silver coatings were prepared by a facile air-spray method on polymer films. Different from the prevailing strategy to endow polyethylene with antibacterial performance, we used metallocene polyethylene sol and nano-silver as a precursor to deposit coatings on polymers at a relatively low operating temperature. Antibacterial coatings with excellent mechanical properties, water resistance, and low silver release were achieved. The composite coatings were examined in terms of surface characteristics, mechanical properties, and antibacterial activity against two representative bacterial strains including Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). The composite coatings exhibited favorable microstructure, good mechanical properties, and suitable crystallinity. The antimicrobial tests indicated that the fabricated composite coatings showed promising antibacterial activity against E. coli and S. aureus. Furthermore, Ag ions released by the composite coating after 30 days were under 1.2 ppb. These results indicated a promising prospect of the composite coating for wide antibacterial applications.     

Evaluation of the Antimicrobial Efficacy of N-Acetyl-l-Cysteine,Rhamnolipids, and Usnic Acid—Novel Approaches to Fight Food-Borne Pathogens

In the food industry, the increasing antimicrobial resistance of food-borne pathogens to conventional sanitizers poses the risk of food contamination and a decrease in product quality and safety. Therefore, we explored alternative antimicrobials N-Acetyl-l-cysteine (NAC), rhamnolipids (RLs), and usnic acid (UA) as a novel approach to prevent biofilm formation and reduce existing biofilms formed by important food-borne pathogens (three strains of Salmonella enterica and two strains of Escherichia coli, Listeria monocytogenes, Staphylococcus aureus). Their effectiveness was evaluated by determining minimum inhibitory concentrations needed for inhibition of bacterial growth, biofilm formation, metabolic activity, and biofilm reduction. Transmission electron microscopy and confocal scanning laser microscopy followed by image analysis were used to visualize and quantify the impact of tested substances on both planktonic and biofilm-associated cells. The in vitro cytotoxicity of the substances was determined as a half-maximal inhibitory concentration in five different cell lines. The results indicate relatively low cytotoxic effects of NAC in comparison to RLs and UA. In addition, NAC inhibited bacterial growth for all strains, while RLs showed overall lower inhibition and UA inhibited only the growth of Gram-positive bacteria. Even though tested substances did not remove the biofilms, NAC represents a promising tool in biofilm prevention.     

A Novel Strategy for Creating an Antibacterial Surface Using a Highly Efficient Electrospray-Based Method for Silica Deposition

Adhesion of bacteria on biomedical implant surfaces is a prerequisite for biofilm formation, which may increase the chances of infection and chronic inflammation. In this study, we employed a novel electrospray-based technique to develop an antibacterial surface by efficiently depositing silica homogeneously onto polyethylene terephthalate (PET) film to achieve hydrophobic and anti-adhesive properties. We evaluated its potential application in inhibiting bacterial adhesion using both Gram-negative Escherichia coli (E. coli) and Gram-positive Staphylococcus aureus (S. aureus) bacteria. These silica-deposited PET surfaces could provide hydrophobic surfaces with a water contact angle greater than 120° as well as increased surface roughness (root mean square roughness value of 82.50 ± 16.22 nm and average roughness value of 65.15 ± 15.26 nm) that could significantly reduce bacterial adhesion by approximately 66.30% and 64.09% for E. coli and S. aureus, respectively, compared with those on plain PET surfaces. Furthermore, we observed that silica-deposited PET surfaces showed no detrimental effects on cell viability in human dermal fibroblasts, as confirmed by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrazolium bromide and live/dead assays. Taken together, such approaches that are easy to synthesize, cost effective, and efficient, and could provide innovative strategies for preventing bacterial adhesion on biomedical implant surfaces in the clinical setting.     

Construction of Er-doped ZnO/SiO2 composites with enhanced antimicrobial properties and analysis of antibacterial mechanism

Herein, silica carrier was used as underlying structure to prepare composite material loaded with rare earth element Er and Zn. Rare earth elements can improve antimicrobial effects of ZnO due to their specific electronic structure. Er–ZnO/SiO₂ hybrid antibacterial material was prepared through sol-gel method and its structure and morphology were characterized by scanning electron microscopy, X-ray diffraction, X-ray photoelectron spectroscopy, inductively coupled plasma emission spectroscopy and Brunauer-Emmett-Teller measurements. E. coli and S. aureus were selected as model bacteria to assess antibacterial activity of prepared hybrid material by plate coating method. Er–ZnO/SiO₂ exhibited good antibacterial activity towards E. coli and S. aureus. Increase in Er³⁺ concentration from 0.12% to 1.10% led to increase in antibacterial performance followed by subsequent decrease. Improving effect of Er relied on the molar ratio of Er doped in ZnO/SiO₂ hybrid material. The optimal sample was found to be 0.60%Er–ZnO/SiO₂, with antibacterial rates of 93.71% and 70.46% against E. coli and S. aureus, respectively. Antibacterial mechanism was assessed by fluorescence detection of reactive oxygen species. In addition, flame atomic absorption spectrometry was used to measure the amount of released Zn²⁺. Results also showed that 0.60%Er–ZnO/SiO₂ hybrid material generated more reactive oxygen species, released more Zn²⁺ ions, and had the largest surface area, which improved its antibacterial rate. Thus, Er enhanced antibacterial properties of ZnO/SiO₂, providing these composite materials with great potential as antibacterial products.     

Effect of Relative Arrangement of Cationic and Lipophilic Moieties on Hemolytic and Antibacterial Activities of PEGylated Polyacrylates

Synthetic amphiphilic polymers have been established as potentially efficient agents to combat widespread deadly infections involving antibiotic resistant superbugs. Incorporation of poly(ethylene glycol) (PEG) side chains into amphiphilic copolymers can reduce their hemolytic activity while maintaining high antibacterial activity. Our study found that the incorporation of PEG has substantially different effects on the hemolytic and antibacterial activities of copolymers depending on structural variations in the positions of cationic centers relative to hydrophobic groups. The PEG side chains dramatically reduced the hemolytic activities in copolymers with hydrophobic hexyl and cationic groups on the same repeating unit. However, in case of terpolymers with cationic and lipophilic groups placed on separate repeating units, the presence of PEG has significantly lower effect on hemolytic activities of these copolymers. PEGylated terpolymers displayed substantially lower activity against Staphylococcus aureus (S. aureus) than Escherichia coli (E. coli) suggesting the deterring effect of S. aureus’ peptidoglycan cell wall against the penetration of PEGylated polymers. Time-kill studies confirmed the bactericidal activity of these copolymers and a 5 log reduction in E. coli colony forming units was observed within 2 h of polymer treatment.     

Eradicating Biofilms of Carbapenem-Resistant Enterobacteriaceae by Simultaneously Dispersing the Biomass and Killing Planktonic Bacteria with PEGylated Branched Polyethyleneimine

Carbapenem-resistant Enterobacteriaceae (CRE) are emerging pathogens that cause variety of severe infections. CRE evade antibiotic treatments because these bacteria produce enzymes that degrade a wide range of antibiotics including carbapenems and β-lactams. The formation of biofilms aggravates CRE infections, especially in a wound environment. These difficulties lead to persistent infection and non-healing wounds. This creates the need for new compounds to overcome CRE antimicrobial resistance and disrupt biofilms. Recent studies in our lab show that 600 Da branched polyethyleneimine (BPEI) and its derivative PEG350-BPEI can overcome antimicrobial resistance and eradicate biofilms in methicillin-resistant S. aureus, methicillin-resistant S. epidermidis, P. aeruginosa, and E. coli. In this study, the ability of 600 Da BPEI and PEG350-BPEI to eradicate carbapenem-resistant Enterobacteriaceae bacteria and their biofilms is demonstrated. We show that both BPEI and PEG350-BPEI have anti-biofilm efficacy against CRE strains expressing Klebsiella pneumoniae carbapenemases (KPCs) and metallo-β-lactamases (MBLs), such as New Delhi MBL (NDM-1). Furthermore, our results illustrate that BPEI affects planktonic CRE bacteria by increasing bacterial length and width from the inability to proceed with normal cell division processes. These data demonstrate the multi-functional properties of 600 Da BPEI and PEG350-BPEI to reduce biofilm formation and mitigate virulence in carbapenem-resistant Enterobacteriaceae.     

Optimization and Evaluation of a Chitosan/Hydroxypropyl Methylcellulose Hydrogel Containing Toluidine Blue O for Antimicrobial Photodynamic Inactivation

Photodynamic inactivation (PDI) combined with chitosan has been shown as a promising antimicrobial approach. The purpose of this study was to develop a chitosan hydrogel containing hydroxypropyl methylcellulose (HPMC), chitosan and toluidine blue O (TBO) to improve the bactericidal efficacy for topical application in clinics. The PDI efficacy of hydrogel was examined in vitro against the biofilms of Staphylococcus aureus (S. aureus) and Pseudomonas aeruginosa (P. aeruginosa). Confocal scanning laser microscopy (CSLM) was performed to investigate the penetration level of TBO into viable S. aureus biofilms. Incorporation of HMPC could increase the physicochemical properties of chitosan hydrogel including the hardness, viscosity as well as bioadhesion; however, higher HMPC concentration also resulted in reduced antimicrobial effect. CSLM analysis further demonstrated that higher HPMC concentration constrained TBO diffusion into the biofilm. The incubation of biofilm and hydrogel was further performed at an angle of 90 degrees. After light irradiation, compared to the mixture of TBO and chitosan, the hydrogel treated sample showed increased PDI efficacy indicated that incorporation of HPMC did improve antimicrobial effect. Finally, the bactericidal efficacy could be significantly augmented by prolonged retention of hydrogel in the biofilm as well as in the animal model of rat skin burn wounds after light irradiation.     

Poly(ε‐caprolactone) composites containing gentamicin‐loaded β‐tricalcium phosphate/gelatin microspheres as bone tissue supports

In this work, novel antibacterial composites were prepared by using poly(ε‐caprolactone) (PCL) as the main matrix material, and gentamicin‐loaded microspheres composed of β‐tricalcium phosphate (β‐TCP) and gelatin. The purpose is to use this biodegradable material as a support for bone tissue. This composite system is expected to enhance bone regeneration by the presence of β‐TCP and prevent a possible infection that might occur around the defected bone region by the release of gentamicin. The effects of the ratio of the β‐TCP/gelatin microspheres on the morphological, mechanical, and degradation properties of composite films as well as in vitro antibiotic release and antibacterial activities against Escherichia coli and Staphylococcus aureus were investigated. The results showed that the composites of PCL and β‐TCP/gelatin microspheres had antibacterial activities for both bacteria. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013     

K88 Fimbrial Adhesin Targeting of Microspheres Containing Gentamicin Made with Albumin Glycated with Lactose

The formulation and characterization of gentamicin-loaded microspheres as a delivery system targeting enterotoxigenic Escherichia coli K88 (E. coli K88) was investigated. Glycated albumin with lactose (BSA-glucose-β (4-1) galactose) was used as the microsphere matrix (MS-Lac) and gentamicin included as the transported antibiotic. The proposed target strategy was that exposed galactoses of MS-Lac could be specifically recognized by E. coli K88 adhesins, and the delivery of gentamicin would inhibit bacterial growth. Lactosylated microspheres (MS-Lac1, MS-Lac2 and MS-Lac3) were obtained using a water-in-oil emulsion, containing gentamicin, followed by crosslinking with different concentrations of glutaraldehyde. Electron microscopy displayed spherical particles with a mean size of 10–17 µm. In vitro release of gentamicin from MS-Lac was best fitted to a first order model, and the antibacterial activity of encapsulated and free gentamicin was comparable. MS-Lac treatments were recognized by plant galactose-specific lectins from Ricinus communis and Sophora japonica and by E. coli K88 adhesins. Results indicate MS-Lac1, produced with 4.2 mg/mL of crosslinker, as the best treatment and that lactosylated microsphere are promising platforms to obtain an active, targeted system against E. coli K88 infections.