title: Liposomal squalenoyl-gemcitabine: formulation, characterization and anticancer activity evaluation.
abstract: A new prodrug of gemcitabine, based on the covalent coupling of squalene to gemcitabine (GemSQ), has been designed to enhance the anticancer activity of gemcitabine, a nucleoside analogue active against a wide variety of tumors. In the present study, the feasibility of encapsulating GemSQ into liposomes either PEGylated or non-PEGylated has been investigated. The in vivo anticancer activity of these formulations has been tested on subcutaneous grafted L1210wt leukemia model and compared to that of free gemcitabine. The liposomal GemSQ appears to be a potential delivery system for the effective treatment of tumors.
authors.affiliation: Université Paris-Sud XI, UMR CNRS 8612, 5 rue J.B. Clément, 92290, Châtenay-Malabry, France.
authors.forename: Barbara
authors.initials: B
authors.lastname: Pili
authors.forename: L Harivardhan
authors.initials: LH
authors.lastname: Reddy
authors.forename: Claudie
authors.initials: C
authors.lastname: Bourgaux
authors.forename: Sinda
authors.initials: S
authors.lastname: Lepêtre-Mouelhi
authors.forename: Didier
authors.initials: D
authors.lastname: Desmaële
authors.forename: Patrick
authors.initials: P
authors.lastname: Couvreur
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage*; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D007938:Leukemia / Q000188:drug therapy; D008081:Liposomes / Q000737:chemistry*; D051379:Mice; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry; D053838:Scattering, Small Angle; D013185:Squalene / Q000737:chemistry*; D014961:X-Ray Diffraction; D000093542:Gemcitabine
chemical_list: D000964:Antimetabolites, Antineoplastic; D008081:Liposomes; D011355:Prodrugs; D003841:Deoxycytidine; D011092:Polyethylene Glycols; D013185:Squalene; D000093542:Gemcitabine