ORBi: Ducat Emilie - The experimental design as practical approach to develop and optimize a formulation of peptide-loaded liposomes

Reference : The experimental design as practical approach to develop and optimize a formulation of p...


	Document type :	Scientific journals : Article
	Discipline(s) :	Human health sciences : Pharmacy, pharmacology & toxicology
	To cite this reference:	http://hdl.handle.net/2268/39720

Title :	The experimental design as practical approach to develop and optimize a formulation of peptide-loaded liposomes
Language :	English
Author, co-author :	Ducat, Emilie [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
	Brion, Michael [ > > ]
	Lecomte, Frédéric [Université de Liège - ULg > Département de pharmacie > Chimie analytique >]
	Evrard, Brigitte [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
	Piel, Géraldine [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
Publication date :	Jun-2010
Journal title :	AAPS PharmSciTech
Publisher :	Amer Assoc Pharmaceutical Scientists
Volume :	11
Issue/season :	2
Pages :	966-975
Audience :	International
ISSN :	1530-9932
City :	Alexandria
Country :	VA
Keywords :	[en] design of experiments ; drug delivery system ; freeze-thawing ; liposomes ; peptide
Abstract :	[en] To investigate the encapsulation of Print 3G, a peptidic agent that could reduce the angiogenic development of breast tumors, pegylated liposomes used as intravenous vectors were studied and characterized. Recently, the path of liposomes has been explored with success to improve the pharmacological properties of peptidic drugs and to stabilize them. In this study, loaded unilamellar vesicles composed of SPC:CHOL:mPEG2000-DSPE (47:47:6) were prepared by the hydration of lipid film technique. An HPLC method was developed and validated for the determination of Print 3G to calculate its encapsulation efficiency. Observed Print 3G adsorption on different materials employed during liposome preparation (such as glass beads, tubing, and connections for extrusion) led to the modification of the manufacturing method. The freeze-thawing technique was used to enhance the amount of Print 3G encapsulated into blank liposomes prepared using the hydration of lipid film procedure. Many factors may influence peptide entrapment, namely the number of freeze-thawing cycles, the lipid concentration, the peptide concentration, and the mixing time. Consequently, a design of experiments was performed to obtain the best encapsulation efficiency while minimizing the number of experiments. The lipid concentration and the number of freeze-thawing cycles were identified as the positive factors influencing the encapsulation. As a result of the optimization, an optimum was found and encapsulation efficiencies were improved from around 30% to 63%. Liposome integrity was evaluated by photon correlation spectroscopy and freeze-fracture electron microscopy to ensure that the selected formulation possesses the required properties to be a potential candidate for further in vitro and in vivo experiments.
Research units :	C.I.R.M.
Funders :	Région wallonne : Direction générale des Technologies, de la Recherche et de l'Energie - DGTRE
Name of the research project :	Peptides antagonistes d'oncoprotéines pour une thérapeutique du cancer du sein
Permalink :	http://hdl.handle.net/2268/39720
DOI :	10.1208/s12249-010-9463-3

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