Liposome and niosome preparation using a membrane contactor for scale-up

Colloids Surf B Biointerfaces. 2012 Jun 1:94:15-21. doi: 10.1016/j.colsurfb.2011.12.036. Epub 2012 Jan 21.

Abstract

The scaling-up ability of liposome and niosome production, from laboratory scale using a syringe-pump device to a pilot scale using the membrane contactor module, was investigated. For this aim, an ethanol injection-based method was applied for liposome and niosome preparation. The syringe-pump device was used for laboratory scale batches production (30 ml for liposomes, 20 ml for niosomes) then a pilot scale (750 ml for liposomes, 1000 ml for niosomes) were obtained using the SPG membrane contactor. Resulted nanovesicles were characterized in terms of mean vesicles size, polydispersity index (PdI) and zeta potential. The drug encapsulation efficiency (E.E.%) was evaluated using two drug-models: caffeine and spironolactone, a hydrophilic and a lipophilic molecule, respectively. As results, nanovectors mean size using the syringe-pump device was comprised between 82 nm and 95 nm for liposomes and between 83 nm and 127 nm for niosomes. The optimal E.E. of caffeine within niosomes, was found around 9.7% whereas the spironolactone E.E. reached 95.6% which may be attributed to its lipophilic properties. For liposomes these values were about 9.7% and 86.4%, respectively. It can be clearly seen that the spironolactone E.E. was slightly higher within niosomes than liposomes. Optimized formulations, which offered smaller size and higher E.E., were selected for pilot scale production using the SPG membrane. It has been found that vesicles characteristics (size and E.E.%) were reproducible using the membrane contactor module. Thus, the current study demonstrated the usefulness of the membrane contactor as a device for scaling-up both liposome and niosome preparations with small mean sizes.

MeSH terms

  • Caffeine / chemistry
  • Drug Compounding
  • Drug Delivery Systems / instrumentation
  • Drug Delivery Systems / methods*
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Infusion Pumps
  • Kinetics
  • Liposomes / chemistry*
  • Liposomes / ultrastructure
  • Microscopy, Electron, Transmission
  • Nanospheres / chemistry*
  • Nanospheres / ultrastructure
  • Particle Size
  • Reproducibility of Results
  • Spironolactone / chemistry

Substances

  • Liposomes
  • Spironolactone
  • Caffeine