Lyophilized Boron Complex Powder for BNCT Solubility
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Solution Overview
Problem
Current boron-containing drugs for boron neutron capture therapy are insoluble and prone to precipitation, limiting their effectiveness and storage stability, necessitating a method to enhance solubility without compromising the boron complex.
Innovation Solution
A lyophilized powder containing a boron complex formed by a dehydration condensation reaction between a dihydroxyboryl compound and a sugar or sugar alcohol, with specific molar ratios and pH conditions, is developed, allowing for improved solubility and stability through complex formation and vacuum drying processes.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If boron-containing drugs are used for boron neutron capture therapy, then tumor cell selectivity is improved, but solubility deteriorates
Solution Approach 1:
The patent uses sugars (glucose, fructose, galactose) and sugar alcohols (sorbitol, mannitol, xylitol) as intermediary molecules to form complexes with dihydroxyboryl compounds. These carbohydrate intermediaries provide hydrophilic groups that enhance water solubility while maintaining the boron-containing therapeutic agent's ability to target tumor cells selectively through the boron neutron capture therapy mechanism.
2Reliability
If boron-containing drugs are formulated for therapy, then therapeutic effectiveness is improved, but storage stability deteriorates
Solution Approach 1:
The patent creates composite materials by forming complexes between dihydroxyboryl compounds and carbohydrates. The composite structure combines the therapeutic boron-containing agent with stabilizing sugar molecules, resulting in a formulation that maintains both therapeutic effectiveness and improved storage stability by preventing precipitation and degradation.
3Quantity of substance
If complex formation is used to improve solubility, then solubility is improved, but manufacturing complexity increases
Solution Approach 1:
The patent segments the manufacturing process into distinct, manageable steps: (1) mixing the dihydroxyboryl compound with sugar or sugar alcohol, (2) allowing spontaneous complex formation through dehydration condensation reaction, and (3) freeze-drying the resulting solution. This segmentation simplifies manufacturing by breaking down the complex formation process into basic, easily controlled operations.
Solution Approach 2:
The complex formation process is designed to occur spontaneously when the dihydroxyboryl compound and carbohydrate are mixed in aqueous solution. The dehydration condensation reaction proceeds automatically under physiological conditions without requiring additional catalysts, energy input, or complex processing equipment, allowing the system to self-assemble the soluble complex.
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 lyophilized powder exhibits excellent solubility, stability, and pH compatibility for physiological applications, maintaining over 99% purity and dissolving quickly in water, making it suitable for boron neutron capture therapy without further processing.
Implementation Method 1
a complex formed by a dehydration condensation reaction of a dihydroxyboryl compound and a sugar or a sugar alcohol
Implementation Method 2
The mixture is immersed into liquid nitrogen to freeze the mixture to form a pre-frozen body
Implementation Method 3
A vacuum drying process is performed to evaporate water from the pre-frozen body to form the lyophilized powder
Implementation Method 4
A vacuum drying process is performed to evaporate water from the pre-frozen body to form the lyophilized powder
Data Source
AI summary
The present disclosure provides a lyophilized powder containing a boron complex. The lyophilized powder includes a sugar acid and a complex formed by a dehydration condensation reaction of a dihydroxyboryl compound and a sugar or a sugar alcohol. The present disclosure also provides a method of forming a lyophilized powder containing a boron complex. The method includes the following operations. A dihydroxyboryl compound and a sugar or a sugar alcohol are mixed to form a mixture, and the mixture includes a complex formed by a dehydration condensation reaction of the dihydroxyboryl compound and the sugar or the sugar alcohol. The mixture is immersed in liquid nitrogen to freeze the mixture to form a pre-frozen body. A vacuum drying process is performed to evaporate water of the pre-frozen body to form a lyophilized powder.