Bioavailability Enhancer
Also known as: Bioenhancers, Absorption enhancers, Drug facilitators, Excipients, Bioavailability Enhancer
Overview
Bioavailability enhancers are substances that increase the absorption or efficacy of a drug or supplement without having significant pharmacological activity themselves at the dose used. They are functional excipients or adjuvants often used in combination with active ingredients to improve absorption and efficacy. Common natural sources include piperine (from black pepper), bile salts (animal-derived), fatty acids (plant and animal sources), and polysaccharides like fenugreek galactomannan. These enhancers work by increasing membrane permeability, inhibiting metabolic enzymes, or protecting active ingredients from degradation. They are used to improve the absorption and bioavailability of poorly absorbed drugs or nutraceuticals, such as curcumin, resveratrol, quercetin, and certain vitamins. Research maturity varies, with strong evidence for some agents like piperine in specific contexts, but limited for others. The quality of available evidence is variable, but promising for specific combinations.
Benefits
Bioavailability enhancers can significantly improve the absorption and efficacy of various compounds. For example, piperine co-supplemented with resveratrol increases resveratrol bioavailability and bioefficacy, leading to improvements in cerebral blood flow and antioxidant effects in animal models. Fenugreek galactomannan-based hydrogel with quercetin has shown a substantial increase in free quercetin bioavailability (18.61-fold) and total quercetin bioavailability (62.08-fold) compared to unformulated quercetin. Sucrosomial® carrier system for vitamin B12 has demonstrated improved absorption and circulatory B12 levels in deficient adults compared to conventional formulations. These enhancers may also reduce the required dose, shorten the treatment period, and minimize toxicity or adverse reactions by improving absorption. They are particularly beneficial for individuals with poor absorption or those taking poorly bioavailable supplements.
How it works
Bioavailability enhancers primarily work by modulating gastrointestinal absorption and first-pass metabolism. They increase membrane permeability using surfactants and fatty acids, inhibit metabolic enzymes like glucuronidation with piperine, and protect active ingredients from degradation through encapsulation in hydrogels. These enhancers interact with enzymes involved in drug metabolism, such as CYP3A4 and UGT enzymes, as well as intestinal transporters and membrane structures. While the enhancers themselves are generally not absorbed in significant amounts, their role is to facilitate the absorption of co-administered compounds, thereby increasing their overall bioavailability and efficacy.
Side effects
Bioavailability enhancers are generally considered safe at recommended doses, especially natural agents like piperine and polysaccharides. Common side effects, occurring in more than 5% of users, may include mild gastrointestinal discomfort such as nausea or diarrhea, particularly in sensitive individuals. Uncommon side effects, affecting 1-5% of users, may involve allergic reactions, although these are rare with natural agents. Rare side effects, seen in less than 1% of users, could include severe hypersensitivity or idiosyncratic reactions. It's important to note that bioavailability enhancers may increase the bioavailability of co-administered drugs, potentially leading to an increased risk of side effects or toxicity. Caution is advised in individuals with known allergies to specific enhancers, and limited data exists for pregnant or lactating women, warranting cautious use in these populations.
Dosage
Dosage varies by agent. For piperine, typical doses range from 5–20 mg per dose, and it is recommended to be taken with curcumin or resveratrol. The dosage for fenugreek galactomannan depends on the formulation, as it is typically used in encapsulation systems. The maximum safe dose is not well established for all agents, but piperine is generally safe up to 20 mg per dose. Bioavailability enhancers should be taken with the active ingredient to maximize absorption. Encapsulated or formulated products with the active ingredient are recommended for best results. Absorption may be enhanced by co-administration with food or specific carriers like Sucrosomial®. No specific cofactors are required, but absorption may be improved with certain dietary fats or carriers.
FAQs
How should bioavailability enhancers be used?
Enhancers should be used in combination with the active ingredient to improve its absorption, not alone. Formulation matters; encapsulated or carrier-based systems are generally more effective.
Are bioavailability enhancers safe?
They are generally safe, but may increase the risk of side effects from co-administered drugs. Consult with a healthcare provider if you have concerns.
When should I take bioavailability enhancers?
Take them with meals or as directed by the formulation instructions to maximize absorption of the active ingredient they are paired with.
What results can I expect from using bioavailability enhancers?
Expect improved absorption and efficacy of the active ingredient, often with a potential reduction in the required dose for the active ingredient.
Are bioavailability enhancers active drugs themselves?
No, enhancers are not active drugs themselves and do not provide benefits when taken alone. They only enhance the absorption of other active compounds.
Research Sources
- https://pmc.ncbi.nlm.nih.gov/articles/PMC3634921/ – This review discusses the concept of bioavailability enhancers, highlighting their role in improving the absorption and efficacy of various drugs and supplements. It covers different types of enhancers and their mechanisms of action, emphasizing their potential to reduce required dosages and minimize adverse effects.
- https://pmc.ncbi.nlm.nih.gov/articles/PMC8470508/ – This review focuses on the co-administration of piperine with resveratrol, demonstrating that piperine enhances resveratrol's bioavailability and bioefficacy. The study highlights improvements in cerebral blood flow and antioxidant effects in animal models, suggesting potential benefits for cognitive and cardiovascular health.
- https://www.mdpi.com/2076-3921/13/3/331 – This systematic review and meta-analysis examines the impact of bioavailability enhancers on curcumin absorption and efficacy. The findings indicate that enhancers like piperine and phospholipids significantly improve curcumin's bioavailability, leading to enhanced therapeutic effects, although heterogeneity in formulations and dosages was noted.
- https://pubs.acs.org/doi/10.1021/acsomega.2c05929 – This study investigates the use of fenugreek galactomannan-based hydrogel formulations to enhance quercetin bioavailability. The results show a substantial increase in both free and total quercetin bioavailability compared to unformulated quercetin, suggesting improved absorption and potential health benefits.
- https://www.frontiersin.org/journals/nutrition/articles/10.3389/fnut.2024.1493593/full – This research explores the use of the Sucrosomial® carrier system to improve vitamin B12 absorption in deficient adults. The study demonstrates that this formulation leads to improved absorption and higher circulatory B12 levels compared to conventional formulations, indicating its potential for addressing B12 deficiency.
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