A Novel Boron Lipid to Modify Liposomal Surfaces for Boron Neutron Capture Therapy

Abstract

Boron neutron capture therapy (BNCT) is a cancer treatment with clinically demonstrated efficacy using boronophenylalanine (BPA) and sodium mercaptododecaborate (BSH). However, tumor tissue selectivity of BSH and retention of BPA in tumor cells is a constant problem. To ensure boron accumulation and retention in tumor tissues, we designed a novel polyethylene glycol (PEG)-based boron-containing lipid (PBL) and examined the potency of delivery of boron using novel PBL-containing liposomes, facilitated by the enhanced permeability and retention (EPR) effect. PBL was synthesized by the reaction of distearoylphosphoethanolamine and BSH linked by PEG with Michael addition while liposomes modified using PBL were prepared from the mixed lipid at a constant molar ratio. In this manner, novel boron liposomes featuring BSH in the liposomal surfaces, instead of being encapsulated in the inner aqueous phase or incorporated in the lipid bilayer membrane, were prepared. These PBL liposomes also carry additional payload capacity for more boron compounds (or anticancer agents) in their inner aqueous phase. The findings demonstrated that PBL liposomes are promising candidates to effect suitable boron accumulation for BNCT.

Particle and Heavy Ion Transport Code System‐Based Microdosimetry for the Development of Boron Agents for Boron Neutron Capture Therapy

“…In contrast, BSH has a high 10 B content per molecule; however, its poor cell membrane permeability has led to its development as a boron agent for BNCT using various DDS. [20][21][22][23] We have previously reported the covalent addition of polyarginine (polyR) to BSH. [8] PolyR confers plasma membrane permeability to BSH, which rapidly translocates from the endosome to the cytoplasm and nucleolus when taken up into the cell via macropinocytosis, and it is retained intracellularly for >24 h. BSH also interacts with a group of RNA-associated proteins in vitro and in situ.…”

Large Scale BN‐perovskite Nanocomposite Aerogel Scintillator for Thermal Neutron Detection

“…Highly sensitive, selective, and stable thermal neutron scintillation detectors have enormous transformational potential for homeland security, resource exploration, clean energy, environmental, aerospace, and other applications. [ 1–9 ] Unlike X( γ )‐rays could be captured by heavy atoms, thermal neutrons are captured only by the specific isotopes such as 3 He, 6 Li, 10 B, and 113 Cd (Figure S1, Supporting Information). Currently, the most successful neutron detector is a 3 He gas‐filled proportional counter owing to its high thermal neutron cross‐section and low density for γ ‐ray response.…”

Gadolinium Neutron Capture Therapy for Cats and Dogs with Spontaneous Tumors Using Gd-DTPA

“…In Japan in 2020, accelerator-based BNCT using the drug Borofalan ® containing boron phenylalanine (BPA) was approved for head and neck cancer treatment in adults, with national insurance coverage [4,5,44]. This has led to even greater public interest in the BNCT technology and a more thorough search for agents that can surpass BPA in efficacy [38,[44][45][46].…”