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TXA497 as a topical antibacterial agent: comparative antistaphylococcal, skin deposition, and skin permeation studies with mupirocin. | LitMetric

TXA497 as a topical antibacterial agent: comparative antistaphylococcal, skin deposition, and skin permeation studies with mupirocin.

Int J Pharm

Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08855, USA; Center for Dermal Research, Life Sciences Building, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA. Electronic address:

Published: December 2014

AI Article Synopsis

  • TXA497 is a new guanidinomethyl biaryl compound that shows strong antibacterial effects against methicillin-resistant Staphylococcus aureus (MRSA), outperforming the traditional treatment mupirocin.
  • The study found that TXA497 has better skin deposition than mupirocin, which means it stays on the skin longer and doesn’t penetrate deeply, reducing the risk of entering the bloodstream.
  • TXA497 was also shown to be non-toxic to human skin cells, presenting it as a promising alternative for treating mupirocin-resistant MRSA skin infections.

Article Abstract

TXA497 is representative of a new class of guanidinomethyl biaryl compounds that exhibit potent bactericidal behavior against methicillin-resistant Staphylococcus aureus (MRSA). In this study, we compared the anti-staphylococcal, skin deposition, and skin permeation properties of TXA497 and the topical anti-MRSA antibiotic mupirocin. The results of minimum inhibitory concentration (MIC) assays revealed that TXA497 retains potent activity against MRSA that is highly resistant to mupirocin. Using Franz diffusion cells, compound deposition into human cadaver skin was evaluated, and the results showed the skin deposition of TXA497 to be significantly greater than that of mupirocin. Moreover, unlike mupirocin, TXA497 does not pass through the entire skin layer, suggesting a minimal potential for the systemic absorption of the compound upon topical administration. Additionally, antibacterial concentrations of TXA497 showed no significant toxicity to primary human keratinocytes. Given the rising levels of mupirocin resistance among MRSA populations, our results are significant in that they highlight TXA497 as a potentially useful alternative therapy for treating MRSA skin infections that are resistant to mupirocin.

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Source
http://dx.doi.org/10.1016/j.ijpharm.2014.09.033DOI Listing

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