title: Carborane derivatives loaded into liposomes as efficient delivery systems for boron neutron capture therapy.
abstract: Boron neutron capture therapy (BNCT) is an anticancer therapy based on the incorporation of (10)B in tumors, followed by neutron irradiation. Recently, the synthesis and delivery of new boronated compounds have been recognized as some of the main challenges in BNCT application. Here, we report on the use of liposomes as carriers for BNCT active compounds. Two carborane derivatives, i.e., o-closocarboranyl beta-lactoside (LCOB) and 1-methyl-o-closocarboranyl-2-hexylthioporphyrazine (H(2)PzCOB), were loaded into liposomes bearing different surface charges. The efficacy of these formulations was tested on model cell cultures, that is, DHD/K12/TRb rat colon carcinoma and B16-F10 murine melanoma. These induce liver and lung metastases, respectively, and are used to study the uptake of standard BNCT drugs, including borophenylalanine (BPA). Boron concentration in treated cells was measured by alpha spectrometry at the TRIGA mark II reactor (University of Pavia). Results showed high performance of the proposed formulations. In particular, the use of cationic liposomes increased the cellular concentration of (10)B by at least 30 times more than that achieved by BPA.
authors: Department of Nuclear and Theoretical Physics, University of Pavia and INFN, Pavia, Italy.
authors: S
authors: S
authors: Altieri
authors: M
authors: M
authors: Balzi
authors: S
authors: S
authors: Bortolussi
authors: P
authors: P
authors: Bruschi
authors: L
authors: L
authors: Ciani
authors: A M
authors: AM
authors: Clerici
authors: P
authors: P
authors: Faraoni
authors: C
authors: C
authors: Ferrari
authors: M A
authors: MA
authors: Gadan
authors: L
authors: L
authors: Panza
authors: D
authors: D
authors: Pietrangeli
authors: G
authors: G
authors: Ricciardi
authors: S
authors: S
authors: Ristori
mesh_terms: D000512:Alpha Particles; D000818:Animals; D001692:Biological Transport; D001880:Boranes / Q000737:chemistry*; D001895:Boron / Q000378:metabolism; D016754:Boron Neutron Capture Therapy; D002244:Carbon / Q000737:chemistry*; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism*; D006027:Glycosides / Q000737:chemistry; D007554:Isotopes; D008081:Liposomes / Q000737:chemistry* / Q000378:metabolism*; D051379:Mice; D051381:Rats; D013057:Spectrum Analysis
chemical_list: D001880:Boranes; D004337:Drug Carriers; D006027:Glycosides; D007554:Isotopes; D008081:Liposomes; C008245:lactosides; D002244:Carbon; D001895:Boron