Abstract
In this report, we propose a new polyborate fragment synthesis strategy along the whole chain of the polysaccharide hyaluronic acid (HA) to produce boron neutron capture therapy (BNCT) compounds. Under high pressure and deformatory solid-state conditions, polymolecular system formation takes place due to association of phase-specific transition components into a more or less distinct microscopic organization. Fourier transform infrared (FTIR) spectroscopy shows that HA and polyborates form a network of cyclic polychelate complexes. HA acts as a multidentate ligand using carboxylic and hydroxyl proton donor groups to link oxygen atoms in B–O–B bonds and borate-anions B–O(−): O–H···O, O–H···(−)O. With free electron pairs in heteroatoms –O(:)···B, –N(:)···B, HA can act simultaneously as an electron donor. Nuclear magnetic resonance (NMR) with 13C and 1H reveals a preserved complex interaction after both solubilizing and attenuating the HA-polyborate system. Stability of the product in water, low cost, ease of synthesis and scalability of manufacturing indicate that HA-polyborate complexes might have advantages over current chemotherapeutic approaches in creating therapeutic agents for BNCT.
Highlights
Great progress has been achieved in the synthesis of boron-10-containing pharmaceutical compounds [1,2,3,4,5,6,7,8,9,10] for boron neutron capture therapy (BNCT)
The data are too complex to discover every facet of the reaction, primary changes in characteristic regions of the spectra in the post-reaction mixture gives a clear path to forming a hypothesis of the interaction
hyaluronic acid (HA) and polyborates can form a net of cyclical polychelate complexes, where HA plays the role of a polydentate ligand
Summary
Great progress has been achieved in the synthesis of boron-10-containing pharmaceutical compounds [1,2,3,4,5,6,7,8,9,10] for boron neutron capture therapy (BNCT). The synthesized compounds can deliver boron-10 to tumour tissues at a concentration of 40 μg/g, which is 3.5 times higher than in normal tissues. These concentrations allow for therapeutic impact on tumours while low background spares normal tissue. Typical synthesis methods using polyhedral boron face an obstacle in the area. Polymers 2018, 10, 181 low background spares normal tissue. Typical synthesis methods using polyhedral boron face an obstacle in the area of biocompatibility. To provide biocompatibility it is necessary to create a system of covalently-bonded elements in one molecule polyhedral architecture is of biocompatibility
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