Effects of Lipid Composition and Preparation Conditions on Physical-Chemical Properties, Technological Parameters and In Vitro Biological Activity of Gemcitabine-Loaded Liposomes

• DOI: 10.2174/156720107779314749
• Publication Date: 2006-12-31T18:28:32Z
• Authors: Maria Grazia Calv...; Christian Celia; Donatella Paolino; Donato Cosco; Michelangelo Iannone; Francesco Castelli; Patrizia Doldo; Massimo Fresta
• Keywords: liposomes; 0301 basic medicine; Antimetabolites, Antineoplastic; Cell Survival; Phosphatidylethanolamines; Static Electricity; Biological Transport; Hydrogen-Ion Concentration; Deoxycytidine; Lipids; Gemcitabine; Polyethylene Glycols; 03 medical and health sciences; Cholesterol; drug delivery; Liposomes; Humans; Technology, Pharmaceutical; Prodrugs; Colloids; pharmacology; Caco-2 Cells; Particle Size; Oleic Acid

The effects of lipid composition and preparation conditions on the physicochemical technological properties gemcitabine-loaded liposomes, as well in vitro anti-tumoral activity various liposome formulations were investigated. Three investigated: DPPC/Chol/Oleic acid (8:3:1 molar ratio, liposomes A), DPPC/Chol/DPPS (6:3:1 B) DPPC/Chol/DSPE-MPEG C). Multilamellar prepared by using TLE, FAT DRV methods, while small unilamellar obtained extrusion through polycarbonate filters. Light scattering techniques used to characterize formulations. Loading capacity release profiles gemcitabine from also Caco-2 cells evaluate antitumoral with respect free drug intracellular uptake. Preparation methods influenced both parameters delivery features. Liposomes a size ranging 200 nm 7 μm obtained. entrapment was higher than that expected probably due an interaction components. following decreasing loading order observed: B > C A. Gemcitabine is modulated two different processes, i.e. desorption permeation liposomal bilayers. MTT assay showed greater cytotoxic effect drug. anticancer observed between formulations: A B. increased correlated ability colloidal carrier increase Due encouraging results high modularity applications potential therapeutic relevance can be envisaged for liposomes. Keywords: Liposomes, cells, gemcitabine, assay, release, activity, uptake