Octreotide labeled aggregates containing platinum complexes as nanovectors for drug delivery.
The synthesis, formulation and a complete physico-chemical characterization, by dynamic light scattering and small angle neutron scattering techniques, of new liposomal aggregates obtained by co-assembling an amphiphilic molecule containing a platinum complex, Peg1500 -Lys(Pt-aminoEtGly)-Lys(C18)2, (abbreviated as (C18)2-PKAG-Pt), with a second amphiphilic monomer, (C18H37)2NCO(CH2)2CO(AdOO)5-Oct ((C18)2 L5-Oct), containing the octreotide bioactive peptide, is reported. Liposomes of (C18)2-PKAG-Pt present a radius of 48 nm, whereas the mixed aggregates (C18)2-PKAG-Pt/(C18)2L5-Oct at 90/10 M ratio give larger liposomes with a radius of 84 nm. In both cases, the bilayer thickness is ~5.3 nm. Encapsulation of doxorubicin in mixed liposomes is also obtained by using the pH gradient method. The obtained liposomes could represent a new target selective cargo system for delivery of cisplatin based drugs and/or doxorubicin on cells overexpressing the sstr2 and sstr5 somatostatin receptors.
CIRPeB, Department of Biological Sciences and IBB CNR, University of Naples Federico II, Napoli, Italy.
Antonella
A
Accardo
Gaetano
G
Mangiapia
Luigi
L
Paduano
Giancarlo
G
Morelli
Diego
D
Tesauro
D000903:Antibiotics, Antineoplastic / Q000737:chemistry*; D018931:Antineoplastic Agents, Hormonal / Q000737:chemistry*; D002945:Cisplatin / Q000737:chemistry*; D004317:Doxorubicin / Q000737:chemistry*; D016503:Drug Delivery Systems; D008081:Liposomes / Q000737:chemistry; D015282:Octreotide / Q000737:chemistry*; D010984:Platinum / Q000737:chemistry*; D017481:Receptors, Somatostatin / Q000819:agonists
D000903:Antibiotics, Antineoplastic; D018931:Antineoplastic Agents, Hormonal; D008081:Liposomes; D017481:Receptors, Somatostatin; C574734:SSTR2 protein, human; D010984:Platinum; D004317:Doxorubicin; C094573:somatostatin receptor 5; D002945:Cisplatin; D015282:Octreotide