[en] Purpose: The purpose of this work is to study the peptide encapsulation into PEGylated liposomes. Two formulations (SPC:CHOL:mPEG-750-DSPE (47:47:6) or SPC:CHOL:mPEG-2000-DSPE (47:47:6)) were investigated.
Methods: Blank SUV liposomes were prepared by the lipid film hydration and the encapsulation was achieved by applying freeze-thawing cycles. Because many factors may influence peptide entrapment (number of freeze-thawing cycles (NC), lipid concentration (LC), peptide concentration (PC), mixing time (MT) and liposome composition (COMP)), a design of experiment (DOE) was performed.
Results: The screening permitted to identify two factors having a positive and significant influence on the encapsulation efficiencies (NC and LC) while the liposome composition had a relatively weak effect. For the second part of the DOE, the positive factors were optimized for liposomes containing mPEG2000. The obtained results revealed a theoretical optimum at 64.75±3.55% when 11 cycles were applied and for the following LC: 36.1mM SPC, 36.1mM CHOL and 4mM mPEG-2000-DSPE. Experimental results showed an encapsulation efficiency of 62.68±2.93%.
Conclusion: The DOE led to significant improvement of encapsulation for liposomes containing mPEG2000. Thereafter, an optimization design for liposomes containing mPEG750 will be started.
Acknowledgements: This work was supported by the Ministry of the Walloon Region.
Research Center/Unit :
C.I.R.M.
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Ducat, Emilie ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Brion, Michael
Evrard, Brigitte ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Piel, Géraldine ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Language :
English
Title :
CHARACTERIZATION AND OPTIMIZATION OF PEPTIDE ENCAPSULATION IN PEGYLATED LIPOSOMES
Publication date :
2009
Number of pages :
A0
Event name :
Pharmscifair
Event place :
Nice, France
Event date :
du 9 au 12 juin 2009
Audience :
International
Name of the research project :
Peptides antagonistes d'oncoprotéines pour une thérapeutique du cancer du sein
Funders :
DGTRE - Région wallonne. Direction générale des Technologies, de la Recherche et de l'Énergie [BE]