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| Note Lecithin and Choline are related Lecithin — a naturally occurring mixture of amphiphilic phospholipids, typically rich in phosphatidylcholine, used extensively as a food-grade emulsifier, solubilizing agent, phospholipid carrier, and bioavailability-enhancing excipient. Standard abbreviation: LEC. Commercial lecithin is commonly derived from soy, sunflower, or egg. Its most therapeutically relevant property is its ability to organize lipids and poorly water-soluble compounds into emulsions, nanoemulsions, liposomes, mixed micelles, and phospholipid complexes, thereby improving dispersion in aqueous environments, protecting susceptible compounds, facilitating gastrointestinal solubilization, and in selected formulations increasing oral absorption and systemic exposure. Primary mechanisms (ranked):
Bioavailability / PK relevance: Lecithin can markedly improve the oral bioavailability of poorly water-soluble compounds when incorporated into optimized phospholipid complexes, oil-in-water emulsions, nanoemulsions, or related lipid delivery systems. Human pharmacokinetic studies have reported approximately 29-fold greater total curcuminoid absorption from a lecithin-based formulation and plasma quercetin exposure up to approximately 20-fold above unformulated quercetin. However, these effects are formulation-specific and should not be interpreted as evidence that simply consuming lecithin together with a compound will reproduce the same enhancement. In-vitro vs systemic exposure relevance: In-vitro digestion models consistently show that lecithin-containing emulsions can increase apparent solubility, micellarization, and bioaccessibility of lipophilic compounds, but improved bioaccessibility does not necessarily translate proportionally into systemic bioavailability. Formulation parameters including lecithin concentration, carrier oil composition, droplet size, gastrointestinal stability, and competing emulsifiers strongly influence the outcome. Human or animal pharmacokinetic evidence is therefore preferred when assigning quantitative enhancement factors. Clinical evidence status: Strong formulation and preclinical evidence; human pharmacokinetic evidence exists for several lecithin/phosphatidylcholine delivery systems. Lecithin itself is not an anticancer therapy, but it is a clinically relevant pharmaceutical and nutraceutical excipient capable of substantially modifying exposure to co-formulated compounds. Lecithin a phospholipid-rich compound (often derived from soy or sunflower), can enhance the bioavailability of certain lipophilic (fat-soluble) and amphipathic compounds by improving their solubility, absorption, and cellular uptake.Supplements and Compounds with Improved Bioavailability via Lecithin Curcumin Up to 20–30x better absorption in some formulations Quercetin Resveratrol Silybin (from milk thistle) Green tea catechins, EGCG Lecithin helps stabilize and protect catechins during digestion Boswellic acids Coenzyme Q10 (CoQ10) Omega-3 fatty acids Vitamin D, E, A, K (Fat-soluble vitamins) Alpha-lipoic acid (ALA) black seed oil (Nigella sativa) and its key active compound, thymoquinone. Lecithin and Phospholipid Bioavailability Enhancement
Interpretation: The strongest human evidence for large lecithin/phosphatidylcholine-associated increases in oral exposure currently exists for curcuminoids, quercetin, berberine and silybin. Animal evidence also supports carnosic acid, CoQ10, resveratrol, puerarin, baicalein, baicalin and several other poorly soluble phytochemicals. Carotenoids, vitamin E, DHA and other lipid-soluble nutrients show strong formulation and gastrointestinal bioaccessibility effects, although the magnitude of systemic enhancement is less consistently established in humans. Important formulation constraint: The values above describe specific engineered phospholipid complexes, phytosomes, nanoemulsions, liposomes or self-emulsifying systems. They should not be interpreted as expected fold increases from simply taking a lecithin capsule with the listed product. For practical oral bioenhancement, lecithin generally performs best when the active compound is dissolved or dispersed with a suitable digestible oil and processed into a stable fine oil-in-water emulsion or phospholipid complex. Lecithin Bioavailability Mechanisms
TSF: P: 0–30 min R: 30 min–3 hr G: >3 hr Alzheimer's disease relevance: Lecithin and phosphatidylcholine have longstanding mechanistic interest in Alzheimer's disease because they provide choline for acetylcholine synthesis and phospholipids for neuronal membranes. Cholinergic dysfunction is an important feature of AD, and oral phosphatidylcholine can increase circulating choline. Preclinical and observational evidence also supports possible effects on membrane integrity, synaptic function and one-carbon metabolism. However, randomized clinical studies of lecithin in established dementia have not shown a clear cognitive or functional benefit. Lecithin should therefore be classified as mechanistically plausible but clinically unproven for AD rather than as an established neuroprotective treatment. |
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| A bioenhancer is an agent capable of enhancing bioavailability and efficacy of a drug with which it is co-administered Query Database for BioEnhancers but the bioenhancers mainly show up under the target notes Bioenhancers - piperine and quercetin are considered bio-enhancers - genistein Piperine act by suppressing P-gp and cytochrome P450 enzymes, which counteract the metabolism of rifampicin via these proteins, thus enhancing the oral bioavailability of rifampicin. It also decreases the intestinal production of glucuronic acid, thus allowing more substances to enter the body in active form. It was found to increase the bioavailability of various drugs from 30% to 200%.[25] Table 1: Published research on bioenhancer effect of piperine with various medicines Drug Studied in Reference Antimicrobial agents Rifampicin In vitro Balakrishnan et al, 2001[11] Isoniazid Rabbits Karan et al, 1998 [12] Pefl oxacin Mountain Gaddi goats Madhukar et al, 2008[13] Tetracycline Rats Atal et al, 1980[14] Sulfadiazine Rats and dogs Atal et al, 1980[14] Oxytetracycline Poultry birds Singh et al, 2005[15] Ampicillin Rabbits Janakiraman and Manavalan, 2008[16] Norfl oxacin Rabbits Janakiraman and Manavalan, 2008 [16] Nevirapine Adult males Kasibhatta et al, 2007 [17] Metronidazole In vitro Singh et al, 2010[18] Analgesics Diclofenac sodium Albino mice Pooja et al, 2007[19] Pentazocine Albino mice Pooja et al, 2007[19] Nimesulide Mice Gupta et al, 1998[20] Antiepileptics Carbamazepine In vitro Pattanaik et al, 2009 [21] Phenytoin Human volunteers Bano et al, 1987[22] Pentobarbitone Rats Majumdar et al, 1990[23] Other drugs Propranolol In vitro Bano et al, 1991 [24] Theophylline In vitro Bano et al, 1991 [24] Nutrients In vitro Pooja et al, 2007 [19 ***Borneol -Borneol is thought to temporarily open tight junctions between endothelial cells, enhancing drug penetration. It may also downregulate efflux transporters such as P-glycoprotein (P-gp), allowing higher intracellular concentrations of co-administered drugs. -presence of urea (as a carrier) increased the aqueous solubility of capsaicin by 3.6-fold compared to pure capsaicin Quercetin is found in citrus fruits and is a dual inhibitor of cytochrome P 3A4 (CYP3A4) and P-gp. Table 2: Effect of quercetin pretreatment/co-treatment on pharmacokinetic parameters of different drugs Drugs combined Increase in pharmacokinetic parametera Cmax AUC ABA Verapamil Two fold Two fold SH Diltiazem SH SH Not known Paclitaxel SH SH T wo fold Digoxin 413% 170% Not known Tamoxifen SH SH 59% Compared to drug in question alone. Cmax, peak plasma concentration; AUC, area under the curve; ABA, absolute bioavailability; SH, significantly higher. Another flavonoid, genistein belongs to the isoflavone class of flavonoids. It is a well-known phytoestrogen. The presence of genistein (10 mg/kg) caused an increase in AUC (54.7%) and a decrease in the total plasma clearance (35.2%) after oral administration of paclitaxel at a dose of 30 mg/kg in rats.[37] Naringin is the major flavonoid glycoside found in grapefruit and makes grapefruit juice taste bitter. Oral naringin (3.3 and 10 mg/kg) was pretreated 30 min before and after intravenous administration of paclitaxel (3 mg/kg), the AUC was significantly improved (40.8% and 49.1% for naringin doses of 3.3 and 10 mg/kg, respectively).[38 Carum carvi/Cuminum cyminum ( Jeera) Carum carvi seeds are a prized culinary herb. Extracts of its parts increased significantly (25%–300%), the bioavailability of a number of classes of drugs, such as antibiotics, antifungals, antivirals, anticancer, cardiovascular, anti-inflammatory/ antiarthritic, anti-TB, antileprosy, antihistaminic/respiratory disorders, corticosteroids, immunosuppressants, and antiulcers. Such extracts either in the presence or absence of piperine have been found to be highly selective in their bioavailability/bioefficacy-enhancing action.[40] Capmul One of the widely used bioenhancers is Capmul MCM C10, a glyceryl monocaprate, produced from edible fats and oils and is commonly used in lip products. In a study in rats, antibiotic ceftriaxone when given concomitantly with capmul, increased the bioavailability of ceftriaxone by 80%.[41] Nitrile glycoside Nitrite glycoside is a bioenhancer for drugs and nutrients. Novel bioactive nitrile glycosides, niaziridin and niazirin is obtained from the leaves, pods, and bark of Moringa oleifera. [42] An immunoenhancing polysaccharide and niaziminin, having structural requirement to inhibit tumor promoter-induced Epstein–Barr virus activation have been reported from the leaves of Moringa.[43,44] It enhances the bioactivity of commonly used antibiotics, such as rifampicin, tetracycline, and ampicillin, and also facilitate the absorption of drugs, vitamins, and nutrients through the gastrointestinal membrane, thus increasing their bioavailability. [41] Niazirin is another bioactive nitrile glycoside belonging to M. oleifera. [45,46] Process of isolation of nitrite glycoside from M. oleifera has been patented (US 6858588) by Khanuja et al in 2004–2005. [42 Mechanism of Action Of Bioenhancers Bioavailability-enhancing activity of natural compounds from the medicinal plants may be attributed to various mechanisms, such as P-gp inhibition activity by flavone, quercetin, and genistein; [51] inhibition of efflux transporters, such as P-gp and breast cancer resistance protein (BCRP),[52,53] by naringin and sinomenine thus preventing drug resistance; DNA receptor binding, modulation of cell signaling transduction, and inhibition of drug efflux pumps[54-56] ; by stimulating leucine amino peptidase and glycyl–glycine dipeptidase activity, thus modulating the cell membrane dynamics related to passive transport mechanism as seen with piperine [57] ; nonspecific mechanisms, such as increased blood supply to the gastrointestinal tract, decreased hydrochloric acid secretion, preventing breakdown of some drugs[6] ; and inhibition of metabolic enzymes participating in the biotransformation of drugs, thus preventing inactivation and elimination of drugs and thereby, increasing their bioavailability. [57-5] |
| 1792- | CUR, | LEC, | Chondroprotective effect of curcumin and lecithin complex in human chondrocytes stimulated by IL-1β via an anti-inflammatory mechanism |
| - | in-vitro, | Arthritis, | RAW264.7 | - | NA, | NA, | HCC-38 |
| 1791- | LEC, | Vegetable lecithins: A review of their compositional diversity, impact on lipid metabolism and potential in cardiometabolic disease prevention |
| - | Review, | Nor, | NA |
| 1793- | LEC, | Unmasking Sunflower Lecithin: Does Science Support the Claims? |
| - | Review, | NA, | NA |
| 8181- | LEC, | CUR, | Soybean lecithin-stabilized oil-in-water (O/W) emulsions increase the stability and in vitro bioaccessibility of bioactive nutrients |
| - | in-vitro, | Nor, | NA |
Query results interpretion may depend on "conditions" listed in the research papers. Such Conditions may include : -low or high Dose -format for product, such as nano of lipid formations -different cell line effects -synergies with other products -if effect was for normal or cancerous cells
Filter Conditions: Pro/AntiFlg:% IllCat:% CanType:% Cells:% prod#:114 Target#:1310 State#:% Dir#:%
wNotes=0 sortOrder:rid,rpid