Efficient method for the production of liposomes containing hydrophilic substances

Efficient encapsulation of hydrophilic small molecules and medium molecular weight drugs such as nucleic acids and peptides in liposomes

Advantage and Core Benefit

  • Size control in the range of 100 nm to several micrometers possible
  • High inclusion rate (~90%) of hydrophilic substances
  • Relatively low cost and easy scale-up due to the simple equipment and liquid treatment process

Background and Technology

There are several methods for liposome production, such as hydration of lipid thin film and ethanol injection, but these methods have some problems, such as low internalization efficiency, size control and difficulty in mass production of hydrophilic liposomes. The inventors have developed a “multiphase emulsion” method, in which (1) an aqueous phase containing a hydrophilic encapsulated substance and an oil phase containing lipid and volatile solvent are first emulsified to obtain uniformly sized W/O emulsion droplets, (2) a W/O/W emulsion is prepared by gradual secondary emulsification, and (3) the solvent is volatilized to below the detection limit by standing in the liquid to obtain liposomes reflecting the emulsion droplet diameter obtained in step (1).

By this method, we succeeded in improving the inclusion rate, size control, and mass production, which were the problems of the conventional technology, and since hydrophilic substances can be efficiently internalized, various applications as liposome carriers are expected.

Data

  • Calcein (>80% inclusion rate), glucose (approx. 60%) and nucleic acids (data not shown) are proven.

Patent

JPB 537103 & US8501204 (Granted)

Researcher

Dr. Sosaku Ichikawa (University of Tsukuba)

Expectations

Development of an optimal liposomalization protocol for the target molecule by joint research. Technology transfer of this liposome technology/know-how by licensing. In order to study this technology, we can provide you with a prototype after you specify (1) the lipid composition, (2) the compounds to be encapsulated, and (3) the particle size.

Product No.WL-03765

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