Development and optimization of a one step process for the production and sterilization of liposomes using supercritical CO2

Int J Pharm. 2024 Feb 15:651:123769. doi: 10.1016/j.ijpharm.2024.123769. Epub 2024 Jan 4.

Abstract

Liposomes are very interesting drug delivery systems for pharmaceutical and therapeutic purposes. However, liposome sterilization as well as their industrial manufacturing remain challenging. Supercritical carbon dioxide is an innovative technology that can potentially overcome these limitations. The aim of this study was to optimize a one-step process for producing and sterilizing liposomes using supercritical CO2. For this purpose, a design of experiment was conducted. The analysis of the experimental design showed that the temperature is the most influential parameter to achieve the sterility assurance level (SAL) required for liposomes (≤10-6). Optimal conditions (80 °C, 240 bar, 30 min) were identified to obtain the fixed critical quality attributes of liposomes. The conditions for preparing and sterilizing empty liposomes of various compositions, as well as liposomes containing the poorly water-soluble drug budesonide, were validated. The results indicate that the liposomes have appropriate physicochemical characteristics for drug delivery, with a size of 200 nm or less and a PdI of 0.35 or less. Additionally, all liposome formulations demonstrated the required SAL and sterility at concentrations of 5 and 45 mM, with high encapsulation efficiency.

Keywords: Encapsulation; Green process; Liposome; One-step process; Production; Quality by design; Sterility assurance level; Sterilization; Supercritical carbon dioxide.

MeSH terms

  • Carbon Dioxide / chemistry
  • Drug Delivery Systems
  • Humans
  • Infertility*
  • Liposomes* / chemistry
  • Sterilization

Substances

  • Liposomes
  • Carbon Dioxide