7beta-hydroxycholesterol lipid formulation for glioblastoma delivery
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Solution Overview
Problem
Current treatments for glioblastoma multiforme (GBM) face challenges such as relapse due to stem cells and the difficulty of chemotherapy molecules crossing the blood-tumour barrier (BTB), leading to insufficient drug delivery to brain tumors.
Innovation Solution
A composition comprising a 7beta-hydroxycholesterol derivative combined with a lipid vehicle, specifically a vegetable oil or mixture of oils, which allows the derivative to cross the BTB and achieve anti-GBM activity in vivo.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional chemotherapy molecules are used, then anti-cancer activity is achieved, but the molecules cannot easily cross the blood-tumour barrier leading to insufficient drug delivery
Solution Approach 1:
The patent changes the chemical parameters of the drug molecule by using 7beta-hydroxycholesterol derivative which has specific stereochemistry and functional groups (hydroxyl group at position 7beta) that enable it to cross the blood-tumour barrier while maintaining anti-cancer activity
Solution Approach 2:
The patent creates a composite formulation by combining the 7beta-hydroxycholesterol derivative with a lipid vehicle (vegetable oil), forming a composition that leverages the lipid solubility of the vehicle to enhance delivery of the therapeutic molecule across the blood-tumour barrier
2Quantity of substance
If liposome or micelle type lipid vehicles are used, then drug delivery is improved, but the formulation complexity increases and administration becomes more difficult
Solution Approach 1:
The patent extracts the essential lipid delivery function from complex liposome/micelle structures and implements it through a simple vegetable oil vehicle, eliminating the need for sophisticated encapsulation systems while maintaining drug delivery efficiency
Solution Approach 2:
The patent uses a simple, inexpensive vegetable oil vehicle instead of complex, expensive liposomal formulations, making the therapy more accessible and easier to administer while achieving comparable or superior results
3Quantity of substance
If high doses of chemotherapy are administered to overcome BTB barrier, then drug delivery to tumour increases, but toxic effects increase
Solution Approach 1:
The patent uses the lipid vehicle (vegetable oil) as an intermediary carrier that facilitates the transport of the 7beta-hydroxycholesterol derivative across the blood-tumour barrier, enabling effective drug delivery at lower doses and thereby reducing toxic effects
Solution Approach 2:
The patent changes the pharmacokinetic parameters of the drug by using the lipid vehicle formulation, which improves bioavailability and tumour penetration, allowing effective treatment at lower doses with reduced toxicity
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 formulation effectively crosses the BTB, ensures sufficient drug delivery to brain tumors, and demonstrates remarkable anti-GBM activity in animal models without causing toxicity, thereby potentially improving treatment outcomes for GBM patients.
Implementation Method 1
said 7beta-hydroxycholesterol derivative is in solution in said lipid vehicle
Data Source
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AI summary
The invention relates to a composition comprising a 7β-hydroxycholesterol derivative and a lipid vehicle, in particular a vegetable oil, and use thereof in the treatment of neoplastic pathologies, such as glioblastoma multiforme. Said composition may be administered by the oral route.