Application Note | Liposomes Verteporfin loading and natural lipids
Both, natural and synthetic lipids are utilized in FDA approved liposomal drug
products. While synthetic lipids are often favoured for their purity, natural
lipids are less costly. In this study, liposomes containing mostly natural lipids
with cholesterol a PEGylated lipid were produced using the NanoAssemblr
microfluidic technology. Microfluidic technology was used to achieve exquisite
control over liposome size and in situ loading of the hydrophobic drug verteporfin.
An encapsulation efficiency of 90% and a limit size of 34 ± 1.5 nm was
achieved with soy-PC formulations. Egg-PC formulations had >80% encapsulation
efficiencies at a size of 39.3 ± 0.9 nm. Interestingly, when substituting a
synthetic PC analog for egg-PC, formulations with the synthetic lipid tended to
aggregate. A possible explanation considering the differences in molecular organization
of saturated and unsaturated PC species is discussed.
Application Note | Liposomes size tuning with system parameters
Liposomes are used as drug carriers to deliver a variety of therapeutic
molecules such as small molecules, proteins and nucleic acids. Liposome size
and homogeneity are crucial factors that affect efficacy of liposomal drugs.
Hence, a liposome production method that streamlines the optimization
of these characteristics will expedite formulation development. Here we
demonstrated the utility of the NanoAssemblr microfluidic technology for
rapidly and reproducibly generating homogeneous liposome populations with
the ability to fine-tune liposome size through computer-controlled parameters.
Bench-scale batches of liposomes were produced at sizes ranging from 40 nm
to 120 nm with exceptional uniformity (polydispersity index, PDI as low as 0.05).
Additionally, the robustness of the NanoAssemblr process was demonstrated
by comparing the size and PDI of 6 independent formulations conducted by
different instrument operators. These data demonstrate how the technology
can be used to expedite development of liposome formulations.
Application Note | Liposomes size tuning with formulation parameters
Liposome encapsulation is a technique that has been used to enhance drug
circulation time and reduce toxicity of hydrophilic molecules, or improve
solubility of hydrophobic molecules. Depending on the type of drug molecule
or target tissue, different liposome compositions are often needed.
Additionally, size and homogeneity of the liposome population can impact
liposome behaviour in vivo. In this application note, we examine the effect
of lipid composition and concentration on the size and size distribution
of liposomes generated using the NanoAssemblrTM Benchtop instrument.
The process reproducibility afforded by the NanoAssemblr Benchtop allows
observed changes in liposome size to be attributed to formulation changes.
Increasing cholesterol content in liposome formulations was found to
increase the size of resulting liposomes.