dodecaborate and Neoplasms

Recent development of boron cluster lipids and their liposomal boron delivery system (BDS) are summarized in this article. Boron compounds used in boron neutron capture therapy (BNCT) are, in general, nontoxic unless neutron capture reaction of boron takes place. Therefore, the boron compounds accumulated into other organs would not cause such side effects for patient. Selective and sufficient delivery of boron-10 to tumor results in the successful BNCT. There are two approaches for BDS: encapsulation of boron compounds into liposomes and incorporation of boron-conjugated lipids into the liposomal bilayer, both of which have been significantly investigated. The combination of both approaches displayed potency and, hence, the ability to reduce the total dose of liposomes without reducing the efficacy of BNCT. Boron compounds that have no affinity to tumor can potentially be delivered to tumor tissues by liposomes, therefore, liposomal BDS would be one of the most attractive approaches for efficient BNCT of various cancers.

Topics: Animals; Boranes; Boron Compounds; Boron Neutron Capture Therapy; Humans; Lipids; Liposomes; Neoplasms; Tissue Distribution

A boron neutron capture therapy (BNCT) system, using boron-10-introduced agents coupled with companion diagnostics, is anticipated as a promising cancer theranostic. Thus, this study aimed to synthesize and evaluate a probe

Topics: Albumins; Animals; Boron Compounds; Boron Neutron Capture Therapy; Cell Line, Tumor; Iodine Radioisotopes; Mice; Neoplasms; Precision Medicine; Tissue Distribution

Water-soluble pteroyl-

Topics: A549 Cells; Boron Compounds; Boron Neutron Capture Therapy; Endocytosis; Folate Receptors, GPI-Anchored; Folic Acid; HeLa Cells; Humans; Nanoconjugates; Neoplasms; Protein Binding

Topics: Animals; Boron; Boron Compounds; Boron Neutron Capture Therapy; Cell Line, Tumor; Drug Carriers; Female; Humans; Integrin alphaVbeta3; Intravital Microscopy; Isotopes; Mice; Neoplasms; Peptides, Cyclic; Serum Albumin, Bovine; Xenograft Model Antitumor Assays

A gas phase binding study revealed strong intrinsic intermolecular interactions between dianionic halogenated closo-dodecaborates [B12X12](2-) and several neutral organic receptors. Oxidation of a tetrathiafulvalene host allowed switching between two host-guest binding modes in a supramolecular complex. Complexes of β-cyclodextrin with [B12F12](2-) show remarkable stability in the gas phase and were successfully tested as carriers for the delivery of boron clusters into cancer cells.

Topics: Anions; Binding Sites; Boron Compounds; Boron Neutron Capture Therapy; Cell Line; Cell Proliferation; Drug Carriers; Drug Delivery Systems; Heterocyclic Compounds; Humans; Hydrophobic and Hydrophilic Interactions; Molecular Structure; Neoplasms; Oxidation-Reduction

Maleimide-conjugating closo-dodecaborate sodium form 5c (MID) synthesized by the nucleophilic ring-opening reaction of closo-dodecaborate-1,4-dioxane complex 2 with tetrabutylammonium (TBA) azide was found to conjugate to free SH of cysteine and lysine residues in BSA under physiological conditions, forming highly boronated BSA that showed high and selective accumulation in tumor and significant tumor growth inhibition in colon 26 tumor-bearing mice subjected to thermal neutron irradiation.

Topics: Animals; Boron; Boron Compounds; Boron Neutron Capture Therapy; Cell Line; Cysteine; Drug Carriers; Female; Lysine; Maleimides; Mice; Mice, Inbred BALB C; Models, Molecular; Neoplasms; Serum Albumin, Bovine

The potential of boron-containing lipids with three different structures, which were intended for use in boron neutron capture therapy, was investigated. All three types of boron lipids contained the anionic dodecaborate cluster as the headgroup. Their effects on two different tumor models in mice following intravenous injection were tested; for this, liposomes with boron lipid, distearoyl phosphatidylcholine, and cholesterol as helper lipids, and containing a polyethylene glycol lipid for steric protection, were administered intravenously into tumor-bearing mice (C3H mice for SCCVII squamous cell carcinoma and BALB/c mice for CT26/WT colon carcinoma). With the exception of one lipid (B-THF-14), the lipids were well tolerated, and no other animal was lost due to systemic toxicity. The lipid which led to death was not found to be much more toxic in cell culture than the other boron lipids. All of the lipids that were well tolerated showed hemorrhage in both tumor models within a few hours after administration. The hemorrhage could be seen by in vivo magnetic resonance and histology, and was found to occur within a few hours. The degree of hemorrhage depended on the amount of boron administered and on the tumor model. The observed unwanted effect of the lipids precludes their use in boron neutron capture therapy.

Topics: Animals; Boron Compounds; Boron Neutron Capture Therapy; Hemorrhage; Histocytochemistry; Lipids; Liposomes; Magnetic Resonance Imaging; Mice; Mice, Inbred BALB C; Neoplasms; Tissue Distribution

New disodium mercaptoundecahydro-closo-dodecaborate (BSH)-conjugated chlorin derivatives 11, 12, 16 and 20 as agents for both photodynamic therapy (PDT) and boron neutron capture therapy (BNCT) of cancer were synthesized. The in vivo biodistribution and clearance of 11, 12, 16 and 20 were investigated in tumor-bearing mice. Compounds 12 and 16 showed good tumor-selective accumulation among the four derivatives. The time to maximum accumulation of compound 16 in tumor tissue was one-fourth of that of compound 12, and clearance from normal tissues of compound 16 was similar to that of compound 12. The in vivo therapeutic efficacy of PDT using 16, which has twice as many boron atoms as 12, was evaluated by measuring tumor growth rates in tumor-bearing mice with 660 nm light-emitting diode irradiation at 6h after injection of 16. Tumor growth was significantly inhibited by PDT using 16. These results suggested that 16 is a good candidate for both PDT and BNCT of cancer.

Topics: Animals; Boron Compounds; Boron Neutron Capture Therapy; Cell Line, Tumor; Cell Survival; Female; Light; Mice; Mice, Inbred BALB C; Neoplasms; Photochemotherapy; Photosensitizing Agents; Porphyrins; Tissue Distribution; Transplantation, Homologous

closo-Dodecaborate-encapsulating liposomes were developed as boron delivery vehicles for neutron capture therapy. The use of spermidinium as a counter cation of closo-dodecaborates was essential not only for the preparation of high boron content liposome solutions but also for efficient boron delivery to tumors.

Topics: Animals; Antineoplastic Agents; Boron; Boron Compounds; Boron Neutron Capture Therapy; Cell Line, Tumor; Cell Survival; Female; Liposomes; Mice, Inbred BALB C; Neoplasms; Tumor Burden

The fluorescence-labeled closo-dodecaborane lipid (FL-SBL) was synthesized from (S)-(+)-1,2-isopropylideneglycerol as a chiral starting material. FL-SBL was readily accumulated into the PEGylated DSPC liposomes prepared from DSPC, CH, and DSPE-PEG-OMe by the post insertion protocol. The boron concentrations and the fluorescent intensities of the FL-SBL-labeled DSPC liposomes increased with the increase of the additive FL-SBL, and the maximum emission wavelength of the liposomes appeared at 531 nm. A preliminary in vivo imaging study of tumor-bearing mice revealed that the FL-SBL-labeled DSPC liposomes were delivered to the tumor tissue but not distributed to hypoxic regions.

Topics: Animals; Boron; Boron Compounds; Drug Delivery Systems; Female; Fluorescence; Liposomes; Mice; Neoplasms; Oxadiazoles; Phosphatidylcholines; Phosphatidylethanolamines; Polyethylene Glycols; Stearates; Tissue Distribution

Closo-dodecaborate lipid liposomes were developed as new vehicles for boron delivery system (BDS) of neutron capture therapy. The current approach is unique because the liposome shell itself possesses cytocidal potential in combination with neutron irradiation. The liposomes composed of closo-dodecaborate lipids DSBL and DPBL displayed high cytotoxicity with thermal neutron irradiation. The closo-dodecaborate lipid liposomes were taken up into the cytoplasm by endocytosis without degradation of the liposomes. Boron concentration of 22.7 ppm in tumor was achieved by injection with DSBL-25% PEG liposomes at 20mg B/kg. Promising BNCT effects were observed in the mice injected with DSBL-25% PEG liposomes: the tumor growth was significantly suppressed after thermal neutron irradiation (1.8 x 10(12)neutrons/cm(2)).

Topics: Animals; Boron; Boron Compounds; Boron Neutron Capture Therapy; Cell Line, Tumor; Drug Delivery Systems; Female; Lipids; Liposomes; Mice; Mice, Inbred BALB C; Microscopy, Electron, Transmission; Neoplasms; Radiopharmaceuticals; Tissue Distribution; Tumor Burden