Resveratrol Transmucosal Delivery Bypasses First-Pass Metabolism
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Solution Overview
Problem
Resveratrol has low bioavailability due to extensive modification by the small intestine and liver during absorption, reducing its effectiveness in achieving desired biological and therapeutic benefits.
Innovation Solution
Compositions comprising resveratrol and a solubilizer, such as sugars like ribose, are administered via oral transmucosal delivery to enhance bioavailability by increasing aqueous solubility and allowing direct absorption through oral mucosal membranes, bypassing first-pass metabolism.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If resveratrol is administered orally through the gastrointestinal tract, then absorption occurs in the duodenum, but extensive modification by the small intestine and liver reduces bioavailability
Solution Approach 1:
The patent extracts resveratrol from the gastrointestinal tract absorption pathway and delivers it directly through the oral mucosa. By using transmucosal delivery formulations (lozenges, tablets, gels), the compound bypasses the duodenum and hepatic first-pass metabolism, extracting it from the conventional oral absorption route to achieve higher bioavailability of parent compound.
Solution Approach 2:
The patent introduces oral mucosal membranes as an intermediary absorption pathway between the administered resveratrol and the systemic circulation. This intermediary route avoids the traditional gastrointestinal tract intermediaries (intestinal enzymes and hepatic metabolism), allowing direct entry into systemic circulation and preventing extensive conjugation.
2Quantity of substance
If resveratrol is administered traditionally orally, then it undergoes glucuronidation and sulfation in the liver, but this reduces the amount of active compound reaching systemic circulation
Solution Approach 1:
The patent extracts resveratrol from the hepatic metabolism pathway by utilizing the oral mucosal route. The formulation delivers the compound directly to the bloodstream through the mouth, extracting it from the liver's conjugating enzymes (glucuronidation and sulfation) before they can modify the compound, thereby preserving active resveratrol in systemic circulation.
Solution Approach 2:
The patent skips the hepatic first-pass metabolism step by using transmucosal delivery. The resveratrol rushes through the oral mucosa barrier and enters systemic circulation directly, bypassing the liver's conjugation processes that would otherwise convert the active compound into inactive derivatives.
3Quantity of substance
If resveratrol is given via conventional oral route, then absorption is limited to approximately 20% in the duodenum, but bioavailability remains low due to first-pass metabolism
Solution Approach 1:
The patent extracts resveratrol from the duodenal absorption pathway and delivers it directly through oral mucosa. This extraction eliminates the time required for intestinal absorption and subsequent hepatic first-pass metabolism, allowing the compound to reach systemic circulation more rapidly and with higher bioavailability.
Solution Approach 2:
The patent skips the sequential process of duodenal absorption followed by hepatic metabolism by using direct transmucosal delivery. The resveratrol rushes through the oral mucosa barrier, bypassing the time-consuming first-pass metabolism that would otherwise occur in the liver before reaching systemic circulation.
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 significantly increases the serum concentration and bioavailability of resveratrol, achieving higher peak plasma levels and extended presence in the serum compared to traditional oral administration, with improved therapeutic efficacy.
Implementation Method 1
Compositions comprising resveratrol and a solubilizer, such as sugars like ribose, are administered via oral transmucosal delivery to enhance bioavailability by increasing aqueous solubility
Implementation Method 2
allowing direct absorption through oral mucosal membranes, bypassing first-pass metabolism
Data Source
AI summary
The present invention relates to compositions and methods comprising resveratrol and uses thereof. Some embodiments include compositions and methods with increased bioavailability of resveratrol. Certain embodiments include compositions comprising resveratrol and a solubilizer. Particular embodiments include transmucosal delivery of resveratrol from the composition.