Carborane Derivatives Loaded into Liposomes as Efficient Delivery Systems for Boron Neutron Capture Therapy

Boron neutron capture therapy (BNCT) is an anticancer therapy based on the incorporation of 10B 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...

Full description

Saved in:
Bibliographic Details
Published in:Journal of medicinal chemistry 2009-12, Vol.52 (23), p.7829-7835
Main Authors: Altieri, S, Balzi, M, Bortolussi, S, Bruschi, P, Ciani, L, Clerici, A. M, Faraoni, P, Ferrari, C, Gadan, M. A, Panza, L, Pietrangeli, D, Ricciardi, G, Ristori, S
Format: Article
Language:English
Subjects:
Alpha Particles
Animals
Biological and medical sciences
Biological Transport
Boranes - chemistry
Boron - metabolism
Boron Neutron Capture Therapy
Carbon - chemistry
Cell Line, Tumor
Drug Carriers - chemistry
Drug Carriers - metabolism
Glycosides - chemistry
Isotopes
Liposomes - chemistry
Liposomes - metabolism
Medical sciences
Mice
Radiation therapy and radiosensitizing agent
Rats
Spectrum Analysis
Treatment with physical agents
Treatment. General aspects
Tumors
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Boron neutron capture therapy (BNCT) is an anticancer therapy based on the incorporation of 10B 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 β-lactoside (LCOB) and 1-methyl-o-closocarboranyl-2-hexylthioporphyrazine (H2PzCOB), 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 α 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 10B by at least 30 times more than that achieved by BPA.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm900763b