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Mapping Fusogenicity of Ciprofloxacin-Loaded Liposomes with Bacterial Cells
Runali Patil1, Arun Torris2, Suresh Bhat2
1Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune, Maharashtra, 411038, India.
Abstract:
The process of liposome fusion with cellular membrane plays key role in delivering encapsulated drug molecule into the cell. This process becomes very important for molecules having low permeability as they fail to reach the site of action located inside the cell. Ciprofloxacin (CIP), a broad-spectrum BCS class IV antibiotic, has poor permeability. In the present work, CIP-loaded liposomes were prepared using solvent evaporation method and optimized by 32 factorial design approach. The optimized batch of CIP-loaded liposomes was characterized for size, entrapment efficiency, zeta potential, FTIR, and microbial susceptibility study on Staphylococcus aureus (gram-positive bacteria) and Escherichia coli (gram-negative bacteria). Confocal microscopy was used to study the fusogenicity process of CIP-loaded liposomes with bacterial cells. Additionally, the kinetics of fusogenicity process was studied using SAXS for the first time. Surprisingly, the rate of fusion of CIP-loaded liposomes with cell wall of S. aureus was twice when compared to the cell wall of E. coli. It is believed that the current work can act as a roadmap in selection of proper excipients while developing formulations which would expedite the fusogenicity and may execute pharmacological activity of poorly penetrable drug molecules at lower dose.
Insights
Liposomes enhance drug delivery by fusing with cell membranes, improving the efficacy of poorly permeable antibiotics like ciprofloxacin. This study optimized liposome formulation and revealed faster fusion with Staphylococcus aureus than Escherichia coli.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Nanotechnology
Background:
- Liposome fusion with cellular membranes is crucial for intracellular drug delivery, especially for poorly permeable drugs.
- Ciprofloxacin (CIP), a broad-spectrum antibiotic, exhibits poor permeability, limiting its intracellular therapeutic potential.
- Developing effective delivery systems is essential to overcome permeability barriers for antibiotics like CIP.
Purpose of the Study:
- To prepare and optimize ciprofloxacin-loaded liposomes using a solvent evaporation method and a 3^2 factorial design.
- To characterize the optimized liposomes for physical, chemical, and biological properties.
- To investigate the fusogenicity of CIP-loaded liposomes with bacterial cells and study the kinetics of this process.
Main Methods:
- Liposomes loaded with ciprofloxacin (CIP) were prepared via solvent evaporation and optimized using a 3^2 factorial design.
- Characterization included size, entrapment efficiency, zeta potential, FTIR, and microbial susceptibility testing against Staphylococcus aureus and Escherichia coli.
- Confocal microscopy and Small-Angle X-ray Scattering (SAXS) were employed to study liposome-cell fusion kinetics.
Main Results:
- Optimized CIP-loaded liposomes were successfully prepared and characterized.
- Liposomes demonstrated susceptibility against both S. aureus and E. coli.
- The fusion rate of CIP-loaded liposomes with the S. aureus cell wall was found to be twice that with the E. coli cell wall.
Conclusions:
- The study successfully developed and optimized ciprofloxacin-loaded liposomes for enhanced drug delivery.
- Liposome fusogenicity with bacterial cell walls varies, with a notably faster rate observed for S. aureus compared to E. coli.
- This research provides a foundation for designing liposomal formulations that enhance the delivery and efficacy of poorly permeable drugs.
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