The effect of ethanol evaporation on the properties of inkjet produced liposomes

Daru. 2020 Jun;28(1):271-280. doi: 10.1007/s40199-020-00340-1. Epub 2020 Apr 18.

Abstract

Background: Inkjet method has been used to produce nano-sized liposomes with a uniform size distribution. However, following the production of liposomes by inkjet method, the solvent residue in the product could have a significant effect on the properties of the final liposomes.

Objective: This research paper aimed to find a suitable method to remove ethanol content and to study its effect on the properties of the final liposomal suspension.

Method: Egg phosphatidylcholine and lidocaine were dissolved in ethanol; and inkjet method at 80 kHz was applied to produce uniform droplets, which were deposited in an aqueous solution to form liposomes. Dry nitrogen gas flow, air-drying, and rotary evaporator were tested to remove the ethanol content. Liposome properties such as size, polydispersity index (PDI), and charge were screened before and after ethanol evaporation.

Results: Only rotary evaporator (at constant speed and room temperature for 2 h) removed all of the ethanol content, with a final drug entrapment efficiency (EE) of 29.44 ± 6.77%. This was higher than a conventional method. Furthermore, removing ethanol led to liposome size reduction from approximately 200 nm to less than 100 nm in most samples. Additionally, this increased the liposomal net charge, which contributed to maintain the uniform and narrow size distribution of liposomes.

Conclusion: Nano-sized liposomes were produced with a narrow PDI and higher EE compared to a conventional method by using an inkjet method. Moreover, rotary evaporator for 2 h reduced effectively the ethanol content, while maintaining the narrow size distribution. Graphical abstract.

Keywords: Ethanol content; Inkjet method; Liposome; Nano- size; PDI; Rotary evaporator.

MeSH terms

  • Drug Liberation
  • Ethanol / chemistry*
  • Ink
  • Liposomes / chemistry*
  • Nanoparticles / chemistry
  • Solvents / chemistry*
  • Technology, Pharmaceutical / methods*
  • Volatilization

Substances

  • Liposomes
  • Solvents
  • Ethanol