Screening of Surfactants for Improved Delivery of Antimicrobials and Poly-Lactic-co-Glycolic Acid Particles in Wound Tissue

Topical wound management is often a challenge due to the poor penetration of antimicrobials in wound tissue and across the biofilm matrix where bacteria are embedded. Surfactants have been used for decades to improve the stability of formulations, increase drug solubility, and enhance penetration. In this study, we screened different detergents with respect to their cytotoxicity and their ability to improve the penetration of poly-lactic-co-glycolic acid (PLGA) particles in wound tissue.

Among the tested surfactants, Kolliphor SLS and Tween 80 increased the penetration of PLGA particles and had a limited cytotoxicity. Then, these surfactants were used to formulate PLGA particles loaded with the poorly water-soluble antibiotic ciprofloxacin. The antimicrobial efficacy of the formulations was tested in a wound infection model based on human ex vivo skin. We found that even though PLGA particles had the same antimicrobial efficiency than the particle-free drug formulation, thanks to their solubilizing and anti-biofilm properties, the surfactants remarkably improved the antimicrobial activity of ciprofloxacin with respect to the drug formulation in water.

We conclude that the use of Tween 80 in antimicrobial formulations might be a safe and efficient option to improve the topical antimicrobial management of chronic wound infections.

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Materials: Poly (d,l-lactide-co-glycolide) 5050 DLG 4A (Evonik Industries, Essen, Germany) and Lumogen (BASF, Ludwigshafen, Germany) was dissolved in acetone with a concentration of 10 mg/mL and 27.77 µg/mL, respectively. This solution is precipitated as nanoparticles against aqueous surfactant solution with a solvent/non-solvent ratio of 1:2. Surfactants used in the production of nanoparticles were Pluronic F68, Pluronic F127, Cremophor RH40, Cremophor A25, Tween 80, Tween 20, Kollidon VA64, Sodium dodecyl sulfate, and PVP 30. All surfactants were purchased from Sigma-Aldrich Chemie, Steinheim, Germany. Two different concentrations of surfactants, 2.5 mg/mL and 10 mg/mL, were used in the aqueous phase. Nanoparticles were prepared by utilizing MJR technology, where ciprofloxacin (Sigma-Aldrich Chemie, Steinheim, Germany) and PLGA are dissolved in DMSO solution (solvent system) and surfactant (either Koliphor SLS or Tween 80) in water solution (non-solvent system) were delivered to the MJR at 1:5 flow rate ratio at 180° angle by using Smartline S100 pumps (Knauer, Munich, Germany) at room temperature. Purification of the nanoparticles was achieved with Continuous Flow Filtration with hollow fiber membranes (Spectrum Labs, MidiCross, 300 KDa) purchased by Repligen (Ravensburg, Germany).

Article information: Rancan, F.; Jurisch, J.; Günday, C.; Türeli, E.; Blume-Peytavi, U.; Vogt, A.; Schaudinn, C.; Günday-Türeli, N. Screening of Surfactants for Improved Delivery of Antimicrobials and Poly-Lactic-co-Glycolic Acid Particles in Wound Tissue. Pharmaceutics 202113, 1093.

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