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Exploring anti-MRSA activity of chitosan-coated liposomal dicloxacillin
Aws Alshamsan1, Fadilah Sfouq Aleanizy1, Mohamed Badran1
1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; Nanobiotechnology Unit, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Abstract:
One of the greatest disturbing global health problems is antibiotic-resistant bacterial infections, which have rendered numerous currently used antibiotics ineffective. Thus, the feasibility of chitosan-coated deformable liposomes (C-Lips) containing dicloxacillin (DLX) were evaluated for their efficacy against methicillin-resistant Staphylococcus aureus (MRSA) strains, which are resistant to beta lactam antibiotics. DLX-loaded liposomes (DLX-Lip) were prepared by a lipid film hydration method and then chitosan (CS) coated (C-DLX-Lip) by the electrostatic deposition method. Both DLX-Lips and C-DLX-Lips showed a particle size distribution with a nano-range and a narrow polydispersity index (PDI). After CS coating, the zeta potential was shifted from negative to positive value. The DLX entrapment efficiency (EE) and drug loading (DL) were 62% and 5.6% for C-DLX-Lips compared to 38% and 3.1% for DLX-Lip, respectively. The in vitro release profile of C-DLX-Lips possessed a slow release behavior. Moreover, the DLX-Lips and C-DLX-Lips demonstrated an enhanced anti-MRSA activity. These results revealed that DLX-Lips and C-DLX-Lips may serve as promising carriers for DLX to increase the efficacy against MRSA, which offers considerably clinical value for long-term use of DLX.
Insights
Chitosan-coated deformable liposomes effectively deliver dicloxacillin, enhancing its efficacy against antibiotic-resistant MRSA strains. This novel drug delivery system shows promise for treating challenging bacterial infections.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Infectious Diseases
Background:
- Antibiotic resistance, particularly from methicillin-resistant Staphylococcus aureus (MRSA), poses a significant global health threat.
- Existing antibiotics are becoming increasingly ineffective against resistant bacterial strains.
- Novel drug delivery systems are crucial for enhancing the efficacy of existing antibiotics.
Purpose of the Study:
- To evaluate the feasibility of chitosan-coated deformable liposomes (C-Lips) for delivering dicloxacillin (DLX).
- To assess the efficacy of DLX-loaded liposomes (DLX-Lips) and C-Lips against MRSA.
- To investigate the physicochemical properties and drug release kinetics of the developed liposomal formulations.
Main Methods:
- DLX-loaded liposomes (DLX-Lips) were prepared using the lipid film hydration method.
- Chitosan coating was applied to DLX-Lips via electrostatic deposition to form C-DLX-Lips.
- Particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency (EE), and drug loading (DL) were characterized.
- In vitro drug release and anti-MRSA activity were evaluated.
Main Results:
- Both DLX-Lips and C-DLX-Lips exhibited nano-range particle size and narrow PDI.
- Chitosan coating shifted zeta potential from negative to positive.
- C-DLX-Lips showed significantly higher DLX entrapment efficiency (62%) and drug loading (5.6%) compared to DLX-Lips (38% and 3.1%).
- C-DLX-Lips demonstrated a sustained in vitro drug release profile.
- Both formulations displayed enhanced anti-MRSA activity.
Conclusions:
- Chitosan-coated deformable liposomes are effective carriers for dicloxacillin.
- These C-Lips enhance DLX efficacy against MRSA, offering potential for improved treatment of resistant infections.
- The developed liposomal system holds considerable clinical value for the long-term use of DLX against MRSA.
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