Reference : PEPTIDE-LOADED LIPOSOMES AGAINST BREAST CANCER: EFFECTIVE PENETRATION IN CELLS OF LONG C...
Scientific congresses and symposiums : Poster
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/73140
PEPTIDE-LOADED LIPOSOMES AGAINST BREAST CANCER: EFFECTIVE PENETRATION IN CELLS OF LONG CIRCULATING pH-SENSITIVE VESICLES
English
Ducat, Emilie mailto [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
Deprez, Julie mailto [Université de Liège - ULg > Département des sciences cliniques > Labo de biologie des tumeurs et du développement >]
Peulen, Olivier mailto [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Département des sciences biomédicales et précliniques >]
Evrard, Brigitte mailto [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
Piel, Géraldine mailto [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
Oct-2010
Yes
No
International
2nd conference on "Innovation in Drug Delivery: From Preformulation to Development through Innovative Evaluation Process"
du 3 au 6 octobre 2010
APGI
Aix-en-Provence
France
[en] Purpose: Print3G, a peptidic antagonist of oncoprotein involved in breast cancer, could reduce the angiogenic development of breast tumors. The necessity of intravenous administration of Print3G led to the development of liposomes as drug carriers, combining the protective properties of PEG with the transfection properties of pH-sensitive lipids. The purpose of this work is to compare pegylated pH-sensitive liposomes with a classical formulation of long-circulating liposomes in terms of cellular uptake. Methods: Classical liposomes (SPC:CHOL:mPEG-750-DSPE (47:47:6 mol/mol)) and pH-sensitive liposomes (DOPE:CHEMS:CHOL: mPEG750-DSPE (43:21:30:6 mol/mol)) were compared in terms of size, charge, stability, pH-sensitivity and toxicity by inhibition of cell proliferation. Finally, confocal microscopy was used to study the cellular uptake of liposomes by three cell lines (Hs578t, WI-26 and MDA-MB-231), using 25-nitrobenzoxydiazol-cholesterol as a fluorescent marker of the vesicular membrane and rhodamine in the inner cavity of liposomes. Results: Sizes of 162.8 ± 4.6 nm and zeta potential of -9.3 ± 1.2 mV were obtained for standard liposomes (n=3) while the obtained values for pH-sensitive liposomes (n=3) were respectively of 184.8 ± 3.2 nm and -19.5 ± 2.6 mV. The two formulations were comparable in terms of shape and stability. Concerning the pH-sensitivity study, a significantly higher leakage of the encapsulated material was observed at pH 5 for pH-sensitive liposomes. Confocal pictures obtained with these vesicles on the three cell lines allowed us to visualize the colocalized red and green color with a higher concentration near the nucleus. Conclusion: Long circulating pH-sensitive liposomes are promising drug delivery systems in terms of cellular uptake. Experiments will be performed with biotinylated Print3G to assess its cellular distribution. Moreover, the accumulation of this formulation in breast tumor will be evaluated by in vivo studies.
C.I.R.M
Région wallonne : Direction générale des Technologies, de la Recherche et de l'Energie - DGTRE
http://hdl.handle.net/2268/73140

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