Biocompatible Nanoparticle CYP Inhibitor for Drug Bioavailability
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Solution Overview
Problem
There is a long-standing need to enhance the bioavailability of pharmaceutical compounds while reducing the first-pass metabolism and variability of blood drug levels, which is essential for optimizing dosage regimens and minimizing adverse reactions.
Innovation Solution
A pharmaceutical composition comprising biocompatible nanoparticles, typically between 4 nm and 100 nm in size, which are administered separately from the pharmaceutical compound of interest, often as inhibitors of human CYP enzymes such as furanocoumarins, to enhance the bioavailability and reduce the required dosage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If standard pharmaceutical doses are administered, then therapeutic efficacy is achieved, but bioavailability is reduced due to first-pass metabolism
Solution Approach 1:
The patent applies preliminary action by administering CYP enzyme inhibitors before the pharmaceutical compound to preemptively block the metabolic pathway. This pre-treatment prevents first-pass metabolism from degrading the compound, thereby improving bioavailability and reducing the required dose. The inhibitors are given in advance to ensure they are present in the system when the compound is administered, blocking CYP-mediated degradation before it can occur.
2Reliability
If higher pharmaceutical doses are administered, then bioavailability may be improved, but variability of blood drug levels increases
Solution Approach 1:
The patent uses CYP enzyme inhibitors as intermediary substances that mediate between the pharmaceutical compound and the metabolic system. These inhibitors act as protective intermediaries that block the variable and unpredictable CYP-mediated metabolism, creating a more stable and predictable blood drug level profile. By introducing this intermediary layer, the system achieves more consistent drug exposure without requiring higher doses.
3Reliability
If standard pharmaceutical doses are administered, then treatment coverage is achieved, but adverse drug reactions occur
Solution Approach 1:
The patent converts the potentially harmful effect of CYP enzyme inhibition into a beneficial outcome. By deliberately administering controlled amounts of CYP inhibitors, the system exploits the enzyme inhibition mechanism to protect against the harmful metabolism of the pharmaceutical compound. This transforms what could be a harmful interaction into a protective effect that reduces adverse reactions while maintaining therapeutic efficacy.
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
This approach allows for a reduction of up to 40% in the pharmaceutical compound dosage while maintaining equivalent bioavailability, thereby improving therapeutic efficacy and reducing costs associated with high-impact diseases.
Implementation Method 1
The at least one biocompatible nanoparticle comprises, or consists in, at least one natural compound which is an inhibitor of a human CYP enzyme, such as furanocoumarin
Data Source
AI summary
The present disclosure generally relates to the field of medicine. The present invention more specifically relates to a pharmaceutical composition comprising the combination of (i) at least one biocompatible nanoparticle comprising, or consisting in, at least one natural compound which is an inhibitor of a human CYP enzyme, the longest dimension of said nanoparticle being of at least 4 nm and less than 100 nm, and (ii) at least one compound of interest, typically at least one pharmaceutical compound, to be administered to a subject in need of such at least one compound of interest, wherein the combination of the at least one biocompatible nanoparticle and of the at least one compound of interest potentiates the at least one compound of interest's bioavailability. The at least one biocompatible nanoparticle is to be administered to the subject separately from the at least one compound of interest (preferably before), typically with an interval of between at least about 5 minutes (preferably more than about 5 minutes) and about 72 hours.