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: Barbara Pili, L Harivardhan Reddy, Claudie Bourgaux, Sinda Lepêtre-Mouelhi, Didier Desmaële, Patrick Couvreur
• Journal: Nanoscale (Nanoscale) Vol. 2 Issue 8 Pg. 1521-6 (Aug 2010) ISSN: 2040-3372 [Electronic] England
• PMID: 20820745 (Publication Type: Journal Article)

Chemical References

• Antimetabolites, Antineoplastic
• Liposomes
• Prodrugs
• Deoxycytidine
• Polyethylene Glycols
• Squalene
• Gemcitabine

Topics

• Animals
• Antimetabolites, Antineoplastic (administration & dosage)
• Calorimetry, Differential Scanning
• Chemistry, Pharmaceutical
• Deoxycytidine (administration & dosage, analogs & derivatives, chemistry)
• Leukemia (drug therapy)
• Liposomes (chemistry)
• Mice
• Particle Size
• Polyethylene Glycols (chemistry)
• Prodrugs (administration & dosage, chemistry)
• Scattering, Small Angle
• Squalene (chemistry)
• X-Ray Diffraction
• Gemcitabine