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Antibacterial activity of a berberine nanoformulation.

ABSTRACT: This study describes the preparation of berberine (BBR) in nanoformulation to enhance its solubility and increase its antibacterial effectiveness against hospital-acquired infections. BBR nanoparticles (BBR NPs) were formed by antisolvent precipitation (ASP) using glycerol as a safe organic solvent. UV-vis absorption spectra demonstrated that the solubility of BBR NPs was greatly enhanced compared to that of pure BBR. Glycerol played a role as a stabilizer for BBR NPs through the formation of hydrogen bonds between glycerol and BBR NPs. The prepared BBR NPs have a narrow size distribution with an average diameter of 156 nm at a concentration of 2.0 mg/mL, measured by dynamic light scattering. After nanoformulation, the concentration of BBR NPs could reach up to 5.0 mg/mL, which is much higher than the saturation concentration without treatment. Results show a strongly enhanced antibacterial activity of BBR NPs compared with that of pure BBR at the same concentration. The minimum bactericidal concentration of BBR NPs against methicillin-resistant Staphylococcus aureus and Escherichia coli O157:H7 was found to be 2.0 and 5.0 mg/mL, respectively. Transmission electron microscopy showed that BBR NPs surrounded the bacterial cells and severely damaged the cell walls. Therefore, BBR NPs prepared by ASP appear to be a potential candidate for the treatment of bacterial pathogens.

SUBMITTER: Nguyen HT

PROVIDER: S-EPMC9296985 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature

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Antibacterial activity of a berberine nanoformulation.

Nguyen Hue Thi HT Pham Tuyet Nhung TN Le Anh-Tuan AT Thuy Nguyen Thanh NT Huy Tran Quang TQ Nguyen Thuy Thi Thu TTT

Beilstein journal of nanotechnology 20220711

This study describes the preparation of berberine (BBR) in nanoformulation to enhance its solubility and increase its antibacterial effectiveness against hospital-acquired infections. BBR nanoparticles (BBR NPs) were formed by antisolvent precipitation (ASP) using glycerol as a safe organic solvent. UV-vis absorption spectra demonstrated that the solubility of BBR NPs was greatly enhanced compared to that of pure BBR. Glycerol played a role as a stabilizer for BBR NPs through the formation of hy ...[more]

PMID: 35923171

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Project description:Berberine is an isoquinoline alkaloid isolated from Chinese herbal medicines such as Coptis chinensis. It has many pharmacological actions, such as antibacterial, hypoglycemic, anti-inflammatory, and so on. However, due to the low lipophilicity of berberine, it is difficult to penetrate the bacterial cell membrane and also difficult to be absorbed orally and usually needs a relatively high dose to achieve the ideal effect. The purpose of this study is to transform the structure of berberine in order to improve the bioavailability of berberine and reduce the dosage. Moreover, we introduce a pharmacophore named Canagliflozin, a hypoglycemic drug (which was also found to have potential anti-bacterial activity) into BBR to see whether this new compound has more existed activities. We at first connected berberine with Canagliflozin, to form a new compound (BC) and see whether BC has synergic effects. We use microbroth dilution method to determine the minimum inhibitory concentration of BC, determine the bacterial growth with the enzyme labeling instrument, observe the formation of bacterial biofilm with crystal violet staining method, observe the bacterial morphology with field emission scanning electron microscope, and determine the intracellular protein with SDS-PAGE. The above indicators reflect the damage of BC to bacteria. New compound BC was successfully obtained by chemical synthesis. The minimal inhibitory concentration of compound BC on three bacteria was significantly better than that of berberine and canagliflozin alone and the combination of berberine and canagliflozin. Moreover, compound BC has obvious destructive effect on bacterial morphology and biofilm, and the compound also has destructive effect on intracellular proteins. Therefore, new compound BC has broad-spectrum antibacterial activity and the inhibitory effect of BC might play a role by destroying the integrity of biofilm and the intracellular protein of bacteria. In conclusion, we create a new molecular entity of berberine and Canagliflozin chimera and open up a new prospect for berberine derivatives in the treatment of bacterial infection.

Project description:There is a growing concern among food safety regulators, the food industry, and consumers about foodborne illnesses. To improve food safety and increase shelf life, it is necessary to use natural preservatives. Natural antimicrobials are safer than artificial preservatives because they can prevent microbial resistance while also meeting consumers' demands for healthier food. This study used Berberine to enhance the antibacterial activity of Satureja Khuzistanica essential oil nanoemulsions (SKEO NE) against Staphylococcus aureus (S. aureus) bacteria, making them a promising option as preservatives. Response Surface Methodology (RSM) was employed to determine the optimized Berberine loaded SKEO NE (Berberine/SKEO NE), resulting in a mean droplet size of 88.60 nm at 6.91, 3.21, and 0.08% w/w of surfactant, essential oil, and Berberine, respectively. Berberine utilization in SKEO NE has led to an increase in antibacterial activity. The nanoemulsion samples significantly ruptured the S. aureus bacterial cell membrane, rapidly discharging cell contents. The use of a microfluidic system in tandem based on the conventional approach significantly accelerated this process. Enhancing the interaction between nanodroplets and the bacterial membrane can be achieved through the nanoemulsification process of EOs, which involves modifying their surface characteristics. This enhancement is particularly pronounced when employing microfluidic systems due to their substantial contact surface area. We investigated the potential of using femtosecond laser irradiation at a wavelength of 1040 nm to augment the antibacterial action of nanoemulsions. The combined treatment of laser and nanoemulsions significantly increased the antibacterial effect of nanoemulsions by approximately 15% for each bacterium, suggesting the potential utility of this treatment to bolster the antibacterial activity of nanoemulsions. Bacteria were trapped using optical tweezers for up to 20 min, with bacterial destruction observed starting at 3 min and exhaustive destruction evident after 20 min.

Project description:The prevalence of nosocomial infections due to multidrug resistant (MDR) bacterial strains is associated with high morbidity and mortality. Folk medicine and ethnopharmacological data can provide a broad range of plants with promising antimicrobial activity. Triphala, an Ayurvedic formula composed of three different plants: Terminalia chebula Retz., Terminalia bellirica (Gaertn.) Roxb. (Combretaceae), and Phyllanthus emblica L. (Phyllanthaceae), is used widely for various microbial infections. Various extraction techniques were applied in the extraction of the biologically active constituents of Triphala in order to compare their efficiency. Microwave-assisted extraction (MAE) was shown to be the most efficient method based on yield, extraction time, and selectivity. The Triphala hydroalcoholic extract (TAE) has been chemically characterized with spectroscopic and chromatographic techniques. Triphala hydroalcoholic extract was evaluated alone or with carvacrol. Different drug formulations including cream and nanoemulsion hydrogel were prepared to assess the antimicrobial activity against selected microorganism strains including Gram-positive and Gram-negative bacteria and fungi. We used a lipophilic oil of carvacrol (5 mg/mL) and a hydrophilic TAE (5 mg/mL) ingredient in a dosage form. Two solutions were created: hydrogel containing nanoemulsion as a lipophilic vector dispersed in the gel as a hydrophilic vehicle and a cream formulation, an oil-in-water emulsion. In both cases, the concentration was 250 mg of active ingredient in 50 mL of final formulation. The formulas developed were stable from a physical and chemical perspective. In the nanoemulsion hydrogel, the oil droplet size ranged from 124 to 129 nm, with low polydispersity index (PdI) 0.132 ± 0.013 and negative zeta potential -46.4 ± 4.3 mV. For the cream, the consistency factor (cetyl alcohol and white wax) induced immobilization of the matrix structure and the stability. Triphala hydroalcoholic extract in drug nanoformulation illustrated might be an adjuvant antimicrobial agent for treating various microbial infections.

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Antibacterial activity of a berberine nanoformulation.

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Antibacterial activity of a berberine nanoformulation.

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