An innovative one step green supercritical CO2 process for the production of liposomes co-encapsulating both a hydrophobic and a hydrophilic compound for pulmonary administration.
[en] Budesonide and salbutamol-loaded liposomes were prepared using an innovative one step supercritical CO2 method without any use of organic solvents. Liposomes composed of soybean phosphatidylcholine, cholesterol and PEGylated lipid (65/30/5% (m/m)) were produced with a size less than 200 nm, a PdI within the range of 0.3 and 0.35 and encapsulation efficiency for budesonide and salbutamol reaching to 94% and 40% respectively. The physical stability of the formulation was improved by optimizing a dry form by freeze-drying with trehalose in a 20:1 (trehalose:lipid) ratio and an increase in the percentage of PEGylated lipid from 5% to 15%. This dry form stored at 4 °C maintains 90-110% of the initial concentration of active compounds. The concentration of budesonide and salbutamol after 15 weeks was 522.92 ± 73.01 µg/mL and 144.86 ± 31.22 µg/mL respectively. These concentrations are close to the concentrations of these molecules in the pharmaceutical products Pulmicort® (500 µg/mL of budesonide) and Ventolin® (100 µg/dose). The formulation tested on lung cells, allows a cell viability of 71 ± 6%, which is not significantly different from untreated cells.
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Penoy, Noémie ; Université de Liège - ULiège > Unités de recherche interfacultaires > Centre Interdisciplinaire de Recherche sur le Médicament (CIRM)
Delma, Kouka Luc; Laboratory of Pharmaceutical Technology and Biopharmacy, Development of Nanomedicine, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, Avenue Hippocrate, 15, 4000 Liege, Belgium, Laboratory of Drug Development, Doctoral School of Sciences and Health, University Joseph KI-ZERBO, 03 BP 7021, Ouagadougou 03, Burkina Faso
Tonakpon, Hermane Avohou; Laboratory of Analytical Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, Avenue Hippocrate, 15, 4000 Liege, Belgium
Grignard, Bruno ; Université de Liège - ULiège > Département de chimie (sciences) > Centre d'études et de recherches sur les macromolécules (CERM)
Evrard, Brigitte ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Piel, Géraldine ; Université de Liège - ULiège > Unités de recherche interfacultaires > Centre Interdisciplinaire de Recherche sur le Médicament (CIRM)
Language :
English
Title :
An innovative one step green supercritical CO2 process for the production of liposomes co-encapsulating both a hydrophobic and a hydrophilic compound for pulmonary administration.
The authors would like to acknowledge the FEDER funds with the NANOPHARE project (portefeuille 884148-329407) in which these results were obtained for their financial support and Luc Delma for the help with the hydrolysis and oxidation index analysis.
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