Interaction of cationic partial dendrimers with charged and neutral liposomes

Amphipathic partial dendrimers having three lipidic (C-14) chains coupled to dendritic lysine head groups with eight, 16 or 32 free terminal amino groups have been synthesised by solid-phase peptide synthesis. Liposomes were prepared with positive, negative and neutral charge using the dehydration rehydration method and their interaction with the partial dendrimers studied. The interaction efficiency of the partial cationic dendrimers studied was greater than 88%. Interaction of the cationic partial dendrimer converted liposomes with very low or negative charge into positively charged species. Apparent vesicle size increased with the head size of the partial dendrimer but, in the case of negatively charged liposomes, large changes in properties were observed after ultracentrifugation due to the formation of myelin figures. To investigate the mode of interaction with the: liposomes, adsorption studies were performed by adding the partial dendrimer after the preparation of dehydration-rehydration vesicles. The results indicated that adsorption is inversely proportional to the head size of the partial dendrimer molecules and the extent of adsorption was similar on both positively and negatively charged liposomes. Adsorption produced liposomes with greater or similar zeta potentials to liposomes that incorporated partial dendrimer through the dehydration-rehydration method. Taking account of the different intel action efficiencies, this suggests there is a degree of partial dendrimer entrappment inside the liposomes. (C) 2001 Elsevier Science B.V. All rights reserved.