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

Abstract

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.

Clinical use and applications of a citrate-based antiseptic lavage for the prevention and treatment of PJI

“…While many surfactants are non-ionic in nature, SLS is anionic and has not only shown to be an effective drug vehicle, but has also shown improved antimicrobial properties compared to other surfactants, likely due to its shorter-chain fatty acid ( 47 , 48 ). In fact, Sharma et al explored the intrinsic capabilities of various surfactants in solubilizing lipid membranes in the context of killing gram-negative bacteria and found faster translocation times across peptidoglycans, greater hydrophobic mismatch and membrane thinning, and greater inner membrane poration in the presence of shorter-chain surfactants when compared to those with longer chains ( 47 ).…”