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Evaluation of Antimicrobial Activities of Nanoparticles and Nanostructured Surfaces In Vitro
Published on: April 21, 2023
Gramicidin and chlorhexidine encapsulated in bicontinuous microemulsions: antimicrobial activity performance and
Douglas G Hayes1, Riley Arp2, Doris H D'Souza2
1University of Tennessee, Departments of Biosystems Engineering and Soil Science, 2506 E.J. Chapman Drive, Knoxville, TN 37996-4531 USA.
Abstract:
The utility of bicontinuous microemulsions (BMEs) as carriers of the antimicrobial peptide (AMP) gramicidin D and antiseptic chlorhexidine was investigated for possible topical delivery to chronic wounds. The two water-insoluble solutes dissolved in pre-formed one-phase BMEs of Water/ Polysorbate 80/ Limonene/ Ethanol/ Glycerol and Water/ Aerosol-OT (AOT)/ Polysorbate 85/ Isopropyl Myristate and an AOT/ Polysorbate 85 Winsor-III system, achieving gramicidin and chlorhexidine concentrations of 1.0 (wt)% and 0.5% individually and 0.5% and 0.3% in mixtures at 22oC, respectively. Small-angle neutron scattering measurements demonstrated that both solutes decreased surfactant interfacial activity and increased interfacial fluidity for the Polysorbate 80 system. For the AOT/ Polysorbate systems, ellipsoidal aggregates consisting of gramicidin and likely adsorbed surfactant and oil formed, while chlorhexidine enhanced the surface activity of surfactants. According to bioassays performed on artificial skin, the incorporation of melittin, gramicidin, and chlorhexidine enhanced the bioactivity of BMEs for 24 h treatment against relevant antibiotic-resistant bacteria found on skin relative to controls. Yet, BME treatments were less effective than aqueous melittin control, in contrast to well diffusion bioassays performed previously. The results reflect the strong impact of AMPs and antiseptics on BME structure and dynamics and the complexity of formulating BMEs for optimal antimicrobial activity.
Insights
Bicontinuous microemulsions (BMEs) effectively carried antimicrobial peptides and antiseptics for topical delivery. However, these active agents altered BME structure, impacting overall antimicrobial effectiveness against resistant bacteria.
Area of Science:
- Colloid and Surface Science
- Materials Science
- Pharmaceutical Sciences
Background:
- Antimicrobial peptides (AMPs) and antiseptics are crucial for combating antibiotic-resistant bacteria.
- Bicontinuous microemulsions (BMEs) offer potential as delivery systems for topical applications.
- Understanding the interaction between active agents and BME structure is vital for formulation efficacy.
Purpose of the Study:
- To investigate the utility of BMEs as carriers for gramicidin D (an AMP) and chlorhexidine (an antiseptic).
- To explore the impact of these agents on BME structure and dynamics.
- To evaluate the antimicrobial efficacy of BME formulations against skin-relevant bacteria.
Main Methods:
- Formulation of BMEs with gramicidin D and chlorhexidine in various systems.
- Characterization of BME structure and dynamics using small-angle neutron scattering (SANS).
- Bioassays on artificial skin to assess antimicrobial activity against antibiotic-resistant bacteria.
Main Results:
- Gramicidin D and chlorhexidine were successfully incorporated into BMEs at significant concentrations.
- Both solutes altered BME interfacial properties, decreasing surfactant activity and increasing fluidity in one system, while forming aggregates in others.
- BME formulations containing active agents showed enhanced bioactivity against bacteria, though overall efficacy was less than aqueous controls in some assays.
Conclusions:
- Antimicrobial peptides and antiseptics significantly influence BME structure and dynamics.
- The complex interactions necessitate careful formulation strategies for optimal antimicrobial delivery via BMEs.
- Further research is needed to optimize BME formulations for enhanced topical antimicrobial activity.
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