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Preclinical development of sodium fusidate antibiotic cutaneous spray based on water-free lipid formulation system
Stockholm University, Sweden; Lipidor AB, Sweden.
Stockholm University, Sweden; Lipidor AB, Sweden.
RISE Research Institutes of Sweden, Materials and Production.
RISE Research Institutes of Sweden, Materials and Production. Gothenburg University, Sweden.ORCID iD: 0000-0002-4270-8475
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2022 (English)In: European Journal of Pharmaceutical Sciences, ISSN 0928-0987, E-ISSN 1879-0720, Vol. 176, article id 106250Article in journal (Refereed) Published
Abstract [en]

Topical antibiotics are a key component in the management of mild to moderate skin and soft tissue infections. There are, however, concerns about the emerging bacterial resistance against topical antibacterial agents such as fusidic acid, due to the prolonged treatment period of its marketed dosage forms. Improving the efficacy of topical formulations could potentially shorten the treatment period and avoid the resistance growth. To provide a more effective drug delivery, a water-free lipid-based formulation system (AKVANO®) which can be applied by spraying, has been developed. In the current paper, different formulations containing sodium fusidate were evaluated for their in vitro skin permeability using artificial skin mimicking membranes and antibacterial properties using ex vivo and in vivo skin wound infection models. The novel formulations containing sodium fusidate showed a much higher skin permeation (up to 60% of nominal amount) than the commercially available Fucidin® cream (3%). These formulations also gave a significantly stronger antibacterial effect than Fucidin cream showing a clear dose-response relationship for the sodium fusidate content. A spray product based on the described formulation technology would therefore require a shorter treatment time and thereby lower the risk for the development of bacterial resistance. Spray administration of these formulations provides an even layer on the skin surface from which the solvent quickly evaporates and thereby facilitates a non-touch application where no rubbing is required. © 2022 The Authors

Place, publisher, year, edition, pages
Elsevier B.V. , 2022. Vol. 176, article id 106250
Keywords [en]
Bacterial resistance, Lipid-based formulation, Skin infection models, Skin permeability, Topical antibiotic spray
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:ri:diva-59825DOI: 10.1016/j.ejps.2022.106250Scopus ID: 2-s2.0-85133911562OAI: oai:DiVA.org:ri-59825DiVA, id: diva2:1685682
Note

 Funding text 1: This research was funded by Lipidor AB, Danderyd, Sweden. Ola Flink funded one of the studies in the article.; Funding text 2: The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Jan Holmbäck, Vibhu Rinwa, Puneet Rinwa, Anders Carlsson and Bengt Herslöf reports financial support was provided by Lipidor AB. Jan Holmbäck and Vibhu Rinwa reports a relationship with Lipidor AB that includes: employment and equity or stocks. Puneet Rinwa reports a relationship with Lipidor AB that includes: employment. Anders Carlsson and Bengt Herslöf reports a relationship with Lipidor AB that includes: consulting or advisory and equity or stocks. Jan Holmbäck, Anders Carlsson and Bengt Herslöf has patents published: See patents as separate list issued to Lipidor AB. Jenny Johansson and Joakim Håkansson reports: No declaration of interests.

Available from: 2022-08-04 Created: 2022-08-04 Last updated: 2023-05-22Bibliographically approved

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