Peptide-BSH Complex for Boron Neutron Capture Therapy
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Solution Overview
Problem
Current boron neutron capture therapy (BNCT) faces challenges in safely and efficiently delivering and retaining boron-containing drugs, such as BSH, within cancer cells due to poor cell permeability and lack of specificity, leading to inadequate killing effects and damage to normal cells.
Innovation Solution
A complex is formed by mixing a peptide with hydrophobic and basic amino acid residues with BSH in an aqueous solution, creating a spherical shape with a diameter of 20 nm to 200 nm, allowing direct delivery and retention within cancer cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If BSH is used as a boron-containing drug for BNCT, then the boron delivery efficiency is improved due to high boron content per molecule, but the cell permeability deteriorates because BSH cannot cross the cell membrane
Solution Approach 1:
The patent uses a peptide as an intermediary carrier that facilitates the transport of BSH across the cell membrane. The peptide-BSH complex acts as a mediator, allowing BSH to enter cancer cells through the amino acid transporter while maintaining the high boron content advantage of BSH.
Solution Approach 2:
The patent creates a composite structure by combining peptide and BSH into a peptide-BSH complex. This composite material leverages the cell permeability of the peptide and the high boron content of BSH, achieving both cell penetration and sufficient boron delivery simultaneously.
2Object-affected harmful factors
If BPA is used as a boron-containing drug for BNCT, then the cell permeability is improved through amino acid transporter, but the boron delivery efficiency deteriorates because BPA has only one boron atom per molecule requiring large amounts to be administered
Solution Approach 1:
The patent merges the advantages of both BPA and BSH by creating a peptide-BSH complex. The complex combines the cell permeability mechanism of BPA (amino acid transporter) with the high boron content of BSH (12 boron atoms per molecule), achieving both efficient cell penetration and high boron delivery in a single formulation.
3Quantity of substance
If BSH is administered to achieve high boron content in cancer cells, then the boron delivery efficiency is improved, but the cancer cell specificity deteriorates because BSH leaks from blood vessels and accumulates in interstitial fluid around cells
Solution Approach 1:
The peptide acts as a specific intermediary that targets cancer cells through the amino acid transporter on the cell membrane. This targeted delivery mechanism ensures that BSH is delivered specifically to cancer cells rather than accumulating non-specifically in interstitial fluid, thereby improving cancer cell specificity while maintaining high boron delivery efficiency.
4Quantity of substance
If large amounts of BPA are administered to deliver sufficient boron to cancer cells, then the boron delivery efficiency is improved, but the harm to normal cells increases due to active uptake by aggressively proliferating normal cells
Solution Approach 1:
The peptide-BSH complex creates a new composite delivery system that maintains high boron content (reducing the need for large doses) while the peptide component provides targeted delivery through amino acid transporters. This reduces the overall dosage required and minimizes uptake by normal cells, thereby reducing harm to normal tissues while maintaining effective boron delivery to cancer cells.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The peptide-BSH complex enhances the delivery and retention of BSH in cancer cells, significantly improving the effectiveness of BNCT while minimizing harm to normal cells.
Implementation Method 1
a complex comprising a peptide containing a hydrophobic amino acid residue and a basic amino acid residue and BSH, obtained by mixing the peptide with BSH in an aqueous solution is in a spherical shape having a diameter of about 20 nm to about 200 nm
Implementation Method 2
directly delivered to and retained in a cancer cell
Data Source
AI summary
The present invention provides: a complex of a mercaptoundecahydrodecaborate (BSH) and a peptide, the complex for boron neutron capture therapy (BNCT); a method for producing the complex; and a cancer therapy using the complex.