Microfluidic Preparation and Characterization of Garcinol-Loaded DSPC–Cholesterol Liposomes for Potential Cystic Fibrosis Therapy
Location
Suwanee, GA
Start Date
17-4-2026 12:00 PM
End Date
17-4-2026 1:00 PM
Description
Introduction: Cystic fibrosis (CF) is a genetic disease characterized by chronic airway inflammation, oxidative stress, and persistent pulmonary infections that progressively damage lung tissue. Therapeutic strategies that deliver anti-inflammatory and antioxidant compounds directly to the lungs may help mitigate disease progression. Garcinol, a hydrophobic polyphenol derived from Garcinia indica, possesses anti-inflammatory and antioxidant properties but has limited clinical utility due to poor aqueous solubility and low bioavailability. Liposomal nanocarriers can improve the solubility and delivery of hydrophobic drugs. In this study, garcinol-loaded DSPC–cholesterol liposomes were prepared using a NanoAssemblr microfluidic platform, and the effect of drug loading on particle size, polydispersity index (PDI), zeta potential, and encapsulation efficiency was evaluated.
Methods: Liposomes were prepared using a microfluidic mixing technique with the NanoAssemblr system (Precision Nano Systems, Cytiva). Two formulations were developed with different drug loading levels: (1) DSPC: Cholesterol: Drug-GC (10:4:0.125 w/w/w) and (2) DSPC: Cholesterol: Drug-GC (10:4:0.250 w/w/w). Lipids and garcinol were dissolved in ethanol to form the organic phase, while purified water served as the aqueous phase. Rapid mixing of the two streams within the microfluidic cartridge induced nanoprecipitation and spontaneous liposome formation. The resulting liposomes were characterized for particle size, PDI, zeta potential, and percent encapsulation efficiency (%EE). Particle size and PDI were determined using dynamic light scattering, while zeta potential was measured to evaluate surface charge and colloidal stability. Encapsulation efficiency was determined after separation of the free drug from the liposome- associated drug. All measurements were performed in triplicate (n=3), and results were expressed as mean ± standard deviation.
Results: The microfluidic process produced nanosized liposomes with relatively narrow size distributions for both formulations. Formulation 1 (10:4:0.125) produced liposomes with an average particle size of 73.87 ± 1.65 nm and a PDI of 0.064 ± 0.065, indicating a highly uniform particle population. The zeta potential was −7.82 ± 2.08 mV, suggesting a slightly negative surface charge typical of DSPC-based liposomes. The encapsulation efficiency was 68 ± 4%. Increasing the drug loading in formulation 2 (10:4:0.250) resulted in a modest increase in particle size to 92.86 nm ±6.86 and a PDI of 0.113 ± 0.088, indicating a slightly broader size distribution. The zeta potential was −9.24 ± 1.61 mV, remaining within a similar, slightly negative range. The encapsulation efficiency was 69 ± 12%, suggesting that increasing the drug content did not significantly affect the liposomal system#39;s drug- loading capacity.
Discussion and Conclusion: Microfluidic preparation using the NanoAssemblr platform successfully produced garcinol-loaded DSPC–cholesterol liposomes with nanoscale particle sizes and narrow size distributions. Increasing drug loading resulted in modest increases in particle size and polydispersity, but did not significantly affect encapsulation efficiency, indicating stable incorporation of garcinol within the lipid bilayer. The slightly negative zeta potential and consistent encapsulation values suggest acceptable colloidal stability of the formulations. Overall, these results demonstrate that microfluidic liposome fabrication is a reliable method for incorporating hydrophobic polyphenols such as garcinol. The developed liposomal system shows potential as a nanocarrier platform for pulmonary delivery of anti-inflammatory agents in cystic fibrosis therapy.
Embargo Period
5-15-2026
Microfluidic Preparation and Characterization of Garcinol-Loaded DSPC–Cholesterol Liposomes for Potential Cystic Fibrosis Therapy
Suwanee, GA
Introduction: Cystic fibrosis (CF) is a genetic disease characterized by chronic airway inflammation, oxidative stress, and persistent pulmonary infections that progressively damage lung tissue. Therapeutic strategies that deliver anti-inflammatory and antioxidant compounds directly to the lungs may help mitigate disease progression. Garcinol, a hydrophobic polyphenol derived from Garcinia indica, possesses anti-inflammatory and antioxidant properties but has limited clinical utility due to poor aqueous solubility and low bioavailability. Liposomal nanocarriers can improve the solubility and delivery of hydrophobic drugs. In this study, garcinol-loaded DSPC–cholesterol liposomes were prepared using a NanoAssemblr microfluidic platform, and the effect of drug loading on particle size, polydispersity index (PDI), zeta potential, and encapsulation efficiency was evaluated.
Methods: Liposomes were prepared using a microfluidic mixing technique with the NanoAssemblr system (Precision Nano Systems, Cytiva). Two formulations were developed with different drug loading levels: (1) DSPC: Cholesterol: Drug-GC (10:4:0.125 w/w/w) and (2) DSPC: Cholesterol: Drug-GC (10:4:0.250 w/w/w). Lipids and garcinol were dissolved in ethanol to form the organic phase, while purified water served as the aqueous phase. Rapid mixing of the two streams within the microfluidic cartridge induced nanoprecipitation and spontaneous liposome formation. The resulting liposomes were characterized for particle size, PDI, zeta potential, and percent encapsulation efficiency (%EE). Particle size and PDI were determined using dynamic light scattering, while zeta potential was measured to evaluate surface charge and colloidal stability. Encapsulation efficiency was determined after separation of the free drug from the liposome- associated drug. All measurements were performed in triplicate (n=3), and results were expressed as mean ± standard deviation.
Results: The microfluidic process produced nanosized liposomes with relatively narrow size distributions for both formulations. Formulation 1 (10:4:0.125) produced liposomes with an average particle size of 73.87 ± 1.65 nm and a PDI of 0.064 ± 0.065, indicating a highly uniform particle population. The zeta potential was −7.82 ± 2.08 mV, suggesting a slightly negative surface charge typical of DSPC-based liposomes. The encapsulation efficiency was 68 ± 4%. Increasing the drug loading in formulation 2 (10:4:0.250) resulted in a modest increase in particle size to 92.86 nm ±6.86 and a PDI of 0.113 ± 0.088, indicating a slightly broader size distribution. The zeta potential was −9.24 ± 1.61 mV, remaining within a similar, slightly negative range. The encapsulation efficiency was 69 ± 12%, suggesting that increasing the drug content did not significantly affect the liposomal system#39;s drug- loading capacity.
Discussion and Conclusion: Microfluidic preparation using the NanoAssemblr platform successfully produced garcinol-loaded DSPC–cholesterol liposomes with nanoscale particle sizes and narrow size distributions. Increasing drug loading resulted in modest increases in particle size and polydispersity, but did not significantly affect encapsulation efficiency, indicating stable incorporation of garcinol within the lipid bilayer. The slightly negative zeta potential and consistent encapsulation values suggest acceptable colloidal stability of the formulations. Overall, these results demonstrate that microfluidic liposome fabrication is a reliable method for incorporating hydrophobic polyphenols such as garcinol. The developed liposomal system shows potential as a nanocarrier platform for pulmonary delivery of anti-inflammatory agents in cystic fibrosis therapy.