Antarctic Brown Algae β-1,3/1,6-Glucan for Soluble Drug Formulations
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Solution Overview
Problem
Existing β-glucans derived from terrestrial sources have inconsistent molecular weight, linkage, and branch distribution, leading to poor water solubility and quality control issues, limiting their effectiveness in cancer immunotherapy and causing side effects like leukocytopenia and thrombocytopenia during chemoradiotherapy.
Innovation Solution
Utilizing β-1,3/1,6-glucan derived from Antarctic brown algae, characterized by specific NMR signals, molecular weight, and solubility, which is prepared through a purification process involving degreasing, aqueous extraction, centrifugation, dialysis, and anion exchange resin purification, enhancing its use in pharmaceutical compositions for treating leukocytopenia and thrombocytopenia.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If β-1,3-glucan is derived from terrestrial sources (barley, oats, edible fungi, yeast), then it can be obtained as a polysaccharide with immune-modulating effects, but the molecular weight, linkage, and degree of branch vary greatly leading to poor water solubility and difficulty in quality control
Solution Approach 1:
The patent changes the source material from terrestrial organisms to Antarctic brown algae, and controls the molecular weight parameter to be 10-500 kDa with specific β-1,3/1,6 linkages. This parameter control resolves the contradiction by achieving both consistent quality (molecular weight 10-500 kDa) and good water solubility, unlike terrestrial sources where high molecular weight (400-800 kDa) causes poor solubility
Solution Approach 2:
The patent specifies particular structural characteristics for different parts of the glucan molecule: β-1,3 linkages forming the main chain with β-1,6 branches at controlled degrees. This local structural control ensures consistent immunomodulatory activity while maintaining solubility through controlled branching patterns
2Reliability
If β-1,3-glucan with high molecular weight (400-800 kDa) is used for injection medicine, then it can provide immune stimulation, but it has poor solubility in water
Solution Approach 1:
The patent optimizes the molecular weight parameter to a specific range of 10-500 kDa, which balances immune stimulation efficacy with water solubility. This resolves the contradiction by showing that extremely high molecular weights (400-800 kDa) are not necessary for immune effect, and the optimized range achieves both goals
3Reliability
If chemoradiotherapy is used to treat cancer, then it can achieve tumor control, but it causes leukocytopenia and thrombocytopenia as side effects
Solution Approach 1:
The patent uses β-1,3/1,6-glucan to convert the harmful effect of chemoradiotherapy (leukocytopenia and thrombocytopenia) into a beneficial outcome. The glucan stimulates immune cell proliferation and differentiation, transforming the therapy-induced immunosuppression into enhanced immune surveillance and protection against infections
Solution Approach 2:
The patent applies β-1,3/1,6-glucan to prevent the harmful side effects of chemoradiotherapy before they fully manifest. By administering the glucan, it preliminarily activates and protects bone marrow hematopoietic cells, preventing the severe leukocytopenia and thrombocytopenia that would otherwise occur during chemoradiotherapy
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 β-1,3/1,6-glucan from Antarctic brown algae demonstrates good water solubility and safety, effectively increasing leukocyte counts, reversing thrombocytopenia, and synergizing with immune checkpoint drugs and chemotherapeutic agents to enhance antitumor effects and reduce side effects.
Implementation Method 1
β-glucans are thought to be pathogen-associated molecular patterns (PAMPs) that regulate host immune responses by triggering innate immune cells such as neutrophils, macrophages and granulocytes
Implementation Method 2
purification process involving degreasing, aqueous extraction, centrifugation, dialysis, and anion exchange resin purification
Data Source
AI summary
An application of a glucan in the preparation of a drug. A β-1,3/1,6-glucan is used for preparing a pharmaceutical composition or formulation. The pharmaceutical composition or formulation can enhance the antitumor effect of immunotherapy, radiotherapy, or chemotherapy, and is used for treating leukopenia and/or thrombocytopenia.