Abstract: The invention relates to methods for obtaining liposomes externally modified with a targeting peptide able to selectively drive liposomal doxorubicin on membrane receptors over expressed in tumours. The invention is based on a kit containing a first vial filled with a sterile, translucent, red dispersion of the liposomal doxorubicin drug; a second vial filled with a modified phospholipid with a reactive function such as DSPE—Peg—maleimide in lyophilized form; and a third vial filled with a peptide modified with an appropriate reactive function, in a 1:1 stoichiometric amount respect to modified phospholipid and in lyophilized form. The kit could also contain an additional fourth vial with the targeting peptide modified with a chelating agent able to complex radioactive metal ions for diagnostic and imaging purposes. The patients to be treated with the peptide modified liposomal doxorubicin could be selected on the basis of the over expression of the targeting receptors.

Abstract: Delivery systems based on liposomes functionalized with peptides and chelating agents, for therapy and imaging by selective targeting of tumour cells expressing the receptors GRP, BB1, BB2, BB3 e BB4 and any other receptor which recognizes the bombesin peptide or analogues thereof are described. In particular, the liposomes contain within them cytotoxic drugs, such as for example doxorubicin, for target-selective antitumour therapy, and, through the presence of the chelating agent, can contain radioactive or paramagnetic ions for the real time visualization of the tumour cells. The liposomes described in this invention thus act as a selective delivery system for drugs and/or contrast agents onto tumour cells expressing the receptors for the class of known peptides such as bombesin (endogenous sequence, analogous or peptidomimetic peptides, agonists or non agonists).

Abstract: The invention relates to supramolecular aggregates obtained by coaggregation of two monomers: —a first monomer containing a paramagnetic or radioactive metal ion complexed by a chelating agent having a lipophilic moiety, —a second monomer containing a bioactive peptide linked to a lipophilic moiety through an organic spacer. The aggregates are selectively driven by the exposed bioactive peptide on a desired biological target. The aggregates (micelles, vesicles or liposomes) could entrap on their inner region or on their surface a pharmaceutical active principle (drug). The invention thus relates to target specific delivery of drugs and/or metal ions. The invention therefore provides compositions containing said aggregates for use as contrast agents, in nuclear medicine or MRI, for the selective delivery of drugs, and for simultaneous delivery of a drug and a metal ion.