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Updated: Jun 19, 2025
Development and Characterization of Fusidic Acid-Loaded Alginate-Aloe vera Based Hydrogel FilmWound Healing
Published on: December 13, 2024
Albumin as a functional carrier solubilizing and facilitating fusidic acid transmembrane delivery into Gram-negative
Xueer Zhou1, Meng Wang1, Yue Wang1
1State Key Laboratory of Oral Diseases & National Center for Stomatology & National Clinical Research Center for Oral Diseases, West China Hospital of Stomatology, Sichuan University, Chengdu 610041, Sichuan, China.
Abstract:
Reversing the bacterial resistance is of great significance and importance. Fusidic acid (FA) is commonly effective against Gram-positive bacterial infections, but most Gram-negative bacteria have intrinsic resistance to FA, primarily due to the strong cell membrane-FA interactions, which highly inhibit the intracellular transport of FA. Herein, we use albumin (bovine serum albumin, BSA) as a bifunctional carrier to solubilize FA and facilitate its transmembrane delivery into Gram-negative bacterial cells. The water solubility of FA is significantly enhanced from 11.87 to 442.20 μg/mL by 5 mg/mL BSA after forming FA-BSA complex. Furthermore, FA-BSA (200 μg/mL) causes 99.96 % viability loss to the model pathogen E. coli upon incubation for 3 h, while free FA or BSA alone shows little activity. Elongation of E. coli cells after treated by FA-BSA is demonstrated by SEM, and the transmembrane transport of FA-BSA is demonstrated by CLSM. Interestingly, increasing the BSA amount substantially reduce the antibacterial activity of FA-BSA, implying an albumin-based transmembrane delivery mechanism may exist. This is the first report regarding successfully reversing the intrinsic resistance of Gram-negative bacteria to FA in the form of FA-BSA. The ready availability of albumin and the simple preparation allows FA-BSA to have great potentials for clinical use.
Insights
Researchers reversed Gram-negative bacterial resistance to fusidic acid (FA) using bovine serum albumin (BSA) as a carrier. FA-BSA complexes enhance FA solubility and transmembrane delivery, overcoming intrinsic bacterial resistance for potential clinical applications.
Area of Science:
- Microbiology
- Biochemistry
- Materials Science
Background:
- Gram-negative bacteria exhibit intrinsic resistance to fusidic acid (FA).
- This resistance is primarily due to cell membrane interactions hindering FA's intracellular transport.
- Developing strategies to overcome this resistance is crucial for treating Gram-negative infections.
Purpose of the Study:
- To investigate the potential of bovine serum albumin (BSA) as a carrier to enhance FA delivery into Gram-negative bacteria.
- To assess the efficacy of FA-BSA complexes in overcoming FA resistance in Gram-negative bacteria.
- To explore the mechanism of FA-BSA mediated transmembrane delivery.
Main Methods:
- Formation of fusidic acid-bovine serum albumin (FA-BSA) complexes.
- Measurement of FA water solubility.
- Antibacterial activity assays against E. coli.
- Scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM) for cell morphology and transport studies.
Main Results:
- BSA significantly increased FA water solubility from 11.87 to 442.20 μg/mL.
- FA-BSA complex (200 μg/mL) achieved 99.96% E. coli viability loss within 3 hours, while free FA or BSA showed minimal activity.
- SEM confirmed E. coli cell elongation post-treatment, and CLSM demonstrated transmembrane transport of FA-BSA.
- Increased BSA concentration reduced antibacterial activity, suggesting an albumin-mediated delivery mechanism.
Conclusions:
- FA-BSA complexes effectively reverse intrinsic Gram-negative bacterial resistance to fusidic acid.
- Albumin acts as a bifunctional carrier, enhancing solubility and facilitating transmembrane delivery.
- The simple preparation and availability of albumin suggest significant potential for FA-BSA in clinical applications against Gram-negative infections.
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