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.
Highlights
Boron neutron capture therapy (BNCT) has attracted considerable attention as a cancer treatment that does not significantly reduce patient quality of life
polyethylene glycol and boron-cluster-modified lipid (PBL) was synthesized by the reaction of distearoylphosphoethanolamine and BSH linked by polyethylene glycol (PEG) with Michael addition while liposomes modified using PBL were prepared from the mixed lipid at a constant molar ratio
The findings demonstrated that PBL liposomes are promising candidates to effect suitable boron accumulation for BNCT
Summary
Boron neutron capture therapy (BNCT) has attracted considerable attention as a cancer treatment that does not significantly reduce patient quality of life. Ligand modification (e.g., carbohydrate chains, peptides, and antibodies) in the case of liposomes can be realized while the cytotoxicity of liposomal materials is extremely low. In this context, by wrapping boron in liposomes, the effectiveness of BNCT can likely be enhanced. The second approach involves the incorporation of lipid-conjugated boron in the liposomal membrane as seen in a report from Hawthorne et al, where they developed a lipid analog with a single carbon chain and a hydrophilic group of nido-carborane [7]. The abovementioned two strategies limit the development of novel drugs that may include additional boron groups To overcome these limitations, we propose a novel drug-delivery strategy based on the outer layer of the liposome membrane. We report on the results of the synthesis of PBL and the properties of the liposomes prepared using this novel lipid
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
