{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,8]],"date-time":"2026-10-08T12:30:36Z","timestamp":1791462636251,"version":"4.3.4"},"reference-count":44,"publisher":"MDPI AG","issue":"10","license":[{"start":{"date-parts":[[2023,10,19]],"date-time":"2023-10-19T00:00:00Z","timestamp":1697673600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"King Saud University, Riyadh, Saudi Arabia","award":["RSP 2023R357"],"award-info":[{"award-number":["RSP 2023R357"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Antibiotics"],"abstract":"<jats:p>Itraconazole (ITZ) is a broad-spectrum antifungal for superficial subcutaneous and systemic fungal infections. This study aimed to enhance the antifungal activity of ITZ using surfactin A (SA), a cyclic lipopeptide produced by the SA-producing Bacillus strain NH-100, possessing strong antifungal activity. SA was extracted, and ITZ-loaded SA micelles formulations were prepared via a single-pot rinsing method and characterized by particle size, zeta potential, and infrared spectroscopy. In vitro dissolution at pH 1.2, as well as hemolysis studies, was also carried out. The fabricated formulations were stable and non-spherical in shape, with an average size of about 179 nm, and FTIR spectra depicted no chemical interaction among formulation components. ITZ-loaded micelles showed decreased hemolysis activity in comparison to pure ITZ. The drug released followed the Korsmeyer\u2013Peppas model, having R2 0.98 with the diffusion release mechanism. In an acidic buffer, drug release of all prepared formulations was in the range of 73\u201389% in 2 h. The molecular simulation showed the outstanding binding and stability profile of the ITZ-SA complex. The aromatic ring of the ITZ mediates a \u03c0-alkyl contact with a side chain in the SA. It can be concluded that ITZ-loaded micelles, owing to significant enhanced antifungal activity up to 6-fold due to the synergistic effect of SA, can be a promising drug delivery platform for delivery of poorly soluble ITZ.<\/jats:p>","DOI":"10.3390\/antibiotics12101550","type":"journal-article","created":{"date-parts":[[2023,10,19]],"date-time":"2023-10-19T07:15:36Z","timestamp":1697699736000},"page":"1550","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":34,"title":["Itraconazole Loaded Biosurfactin Micelles with Enhanced Antifungal Activity: Fabrication, Evaluation and Molecular Simulation"],"prefix":"10.3390","volume":"12","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-8998-9454","authenticated-orcid":false,"given":"Faisal","family":"Usman","sequence":"first","affiliation":[{"name":"Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University, Multan 66000, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0586-3476","authenticated-orcid":false,"given":"Mudassir","family":"Farooq","sequence":"additional","affiliation":[{"name":"Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0008-3498-4112","authenticated-orcid":false,"given":"Tanveer A.","family":"Wani","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5053-5968","authenticated-orcid":false,"given":"Hassan","family":"Ahmad","sequence":"additional","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, University of Central Punjab, 1-Khayaban.e. Jinnah Road, Johar Town, Lahore 54000, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ibrahim","family":"Javed","sequence":"additional","affiliation":[{"name":"Center for Pharmaceutical Innovation, Clinical and Health Sciences, The University of South Australia, North Terrace, Adelaide 5000, Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mazhar","family":"Iqbal","sequence":"additional","affiliation":[{"name":"Health Biotechnology Division, National Institute for Biotechnology and Genetic Engineering (NIBGE), Faisalabad 44000, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fatima Akbar","family":"Sheikh","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Niazi Medical and Dental College, Sargodha 40100, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4358-5259","authenticated-orcid":false,"given":"Farhan","family":"Siddique","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Bahauddin Zakariya University, Multan 66000, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5622-0841","authenticated-orcid":false,"given":"Seema","family":"Zargar","sequence":"additional","affiliation":[{"name":"Department of Biochemistry, College of Sciences, King Saud University, P.O. Box 22452, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Saleh","family":"Sheikh","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University, Multan 66000, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2023,10,19]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","unstructured":"Kangabam, N., and Nethravathy, V. (2023). An overview of opportunistic fungal infections associated with COVID-19. 3 Biotech, 13.","DOI":"10.1007\/s13205-023-03648-2"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"396","DOI":"10.3390\/jof9040396","article-title":"Relationship of Sporotrichosis and Infected Patients with HIV-AIDS: An Actual Systematic Review","volume":"9","author":"Arenas","year":"2023","journal-title":"J. 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