The emergence of antibiotic resistance over the past several decades has given urgency to new antibacterial strategies that apply less selective pressure. A new class of anti-virulence compounds were developed that are active against methicillin-resistant Staphylococcus aureus (MRSA), by inhibiting bacterial virulence without hindering their growth to reduce the selective pressure for resistance development. One of the compounds CCG-211790 has demonstrated potent anti-biofilm activity against MRSA. This new class of anti-virulence compounds inhibited the gene expression of virulence factors involved in biofilm formation and disrupted the biofilm structures. In this study, the physicochemical properties of CCG- 211790, including morphology, solubility in pure water or in water containing sodium dodecyl sulfate, solubility in organic solvents, and stability with respect to pH were investigated for the first time. Furthermore, a topical formulation was developed to enhance the therapeutic potential of the compound. The formulation demonstrated acceptable properties for drug release, viscosity, pH, cosmetic elegance and stability of over nine months.
N. Wang and F. Qi and H. Yu and B. D. Yestrepsky and S. D. Larsen and H. Shi and J. Ji and D. W. Anderson and H. Li and H. Sun, "Physicochemical Properties and Formulation Development of a Novel Compound Inhibiting Staphylococcus Aureus Biofilm Formation," PLoS ONE, vol. 16, Public Library of Science, Feb 2021.
The definitive version is available at https://doi.org/10.1371/journal.pone.0246408
Keywords and Phrases
Bacterial biofilms; Solubility; Staphylococcus aureus; Antibiotic resistance; Vegetable oils; Organic solvents; Virulence factors; Bacterial pathogens
International Standard Serial Number (ISSN)
Article - Journal
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01 Feb 2021