Review article published in a magazine Antioxidant We provide a detailed overview of nanoparticle-based strategies to improve curcumin bioavailability and bioactivity.
Research: Enhancing the bioavailability and bioactivity of curcumin for disease prevention and treatment. Image credit: Microgen / Shutterstock
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Curcumin, the main bioactive compound in turmeric, is a polyphenol found in turmeric. Curcumalonga roots. This compound has numerous health benefits, including anti-cancer, antioxidant, anti-inflammatory, anti-obesity, anti-diabetic, anti-bacterial, wound-healing and hypolipidemic properties.
Curcumin has low bioavailability in human organs and is quickly converted into many bioactive metabolites after absorption from the intestine.Dried turmeric powder prepared from Curcumalonga The roots contain about 2-5% curcumin.
Curcumin ingested from dietary sources is sufficient to influence the intestinal flora. However, due to rapid metabolism, intact curcumin concentrations in the circulation are very low (submicromolar concentrations) and insufficient to trigger cell signaling or gene expression. in vitro Research using cultured cells.
Example of curcumin nano-delivery system.
Strategies to increase curcumin bioavailability
Dietary curcumin is inefficiently absorbed across the intestinal epithelium and undergoes rapid metabolism and systemic excretion. In aqueous solutions at neutral pH, the enol state of curcumin is formed, reducing the stability of curcumin.
Several nanoformulations have been developed to increase curcumin concentrations in the circulation and within specific cells, tissues, and organelles. These nanoformulations are designed to increase the solubility of curcumin, improve its stability during gastrointestinal absorption, alter the absorption route, and inhibit detoxifying enzymes using adjuvants.
The latest generation of curcumin nanoformulations can increase the bioavailability of free curcumin in plasma more than 100 times, improving absorption, cellular uptake, blood-brain barrier permeability, and tissue distribution.
Factors that improve the bioavailability of curcumin include nanoparticle composition, size, and route of administration. Curcumin formulations containing nanoparticles of smaller size have been found to have increased bioavailability when administered orally. In contrast, larger sized nanoparticles have been found to increase bioavailability when administered intravenously.
Curcumin nanoformulations are capable of inducing senescence in malignant and normal cells, thus contributing to various types of cancer and age-related diseases, including cardiometabolic diseases, neurodegenerative diseases, liver, lung, and gastrointestinal diseases. can be effectively treated.
Regarding its mechanism of action, existing evidence suggests that curcumin acts as an antioxidant and anti-inflammatory compound to reduce the production of reactive oxygen species (ROS) and modulate cell signaling and gene expression associated with inflammatory pathways. It shows that. These activities work synergistically to maintain the homeostasis of cellular macromolecules (proteins, DNA, and lipids).
These activities can be enhanced by incorporating curcumin into nanoparticle-based formulations such as polymeric curcumin-bioperine-PLGA. Isomerization of curcumin to cis-trans curcumin is known to increase its ability to bind to adenosine receptors. Incorporation of cis-trans curcumin into nanoformulations is considered to be a valuable strategy to enhance therapeutic efficacy against inflammatory diseases.
Regarding the safety profile, recent clinical trials have shown that the majority of curcumin nanoformulations are well-tolerated and safe for human use.
Antibacterial action
Curcumin is known to exert antibacterial effects against both Gram-positive and Gram-negative bacteria, and this activity is beneficial for topical applications against skin infections as well as for oral and intestinal applications. Additionally, curcumin can indirectly prevent infections by inhibiting the growth of bacteria in food.
The antibacterial activity of curcumin can be enhanced by incorporating curcumin into nanoformulations. Administering curcumin with other compounds such as antibiotics, honey, and other polyphenols may enhance its antibacterial and biofilm-inhibiting effects.
Effect of curcumin nanoformulation on gastrointestinal tract
Several nanotechnology-based systems such as micelles, liposomes, exosomes, phospholipid complexes, nanoemulsions, nanostructured lipid carriers, and biopolymer nanoparticles have been found to enhance the bioavailability of oral curcumin. .
Nanoparticle curcumin, called 'Theracurmin', was found to suppress colitis in mice by regulating the intestinal flora. An improvement in the composition of the intestinal microbiota was also achieved using nanobubble curcumin extract. Curcumin loaded with nanostructured lipid carriers has been shown to reduce colonic inflammation in animals.
Incorporation of curcumin into liposomes has been shown to improve gastrointestinal absorption and enhance its anticancer activity. Additionally, administering curcumin together with other bioactive compounds such as piperine and salsalate has been shown to increase the bioavailability and bioactivity of curcumin.
Effect of curcumin nanoformulation on liver and adipose tissue
Nanoformulations of curcumin with adjuvants such as piperine and quercetin have been found to significantly enhance its bioavailability and bioactivity. Various nanotechnology-based delivery systems such as micelles, liposomes, polymeric nanoparticles, metal nanoparticles, and solid lipid nanoparticles have been found to enhance the bioavailability of curcumin.
Curcumin's anti-inflammatory, antioxidant, and antifibrotic properties make it a potential therapeutic compound for liver diseases. In liver diseases, curcumin nanoformulations have been found to enhance therapeutic efficacy by increasing curcumin solubility, bioavailability, membrane permeability, and improving pharmacokinetics, pharmacodynamics, and biodistribution.
Effect of curcumin nanoformulation on cardiovascular system
Curcumin encapsulated in carboxymethyl chitosan nanoparticles conjugated to a myocyte-specific homing peptide was found to enhance the bioavailability of curcumin in the heart. This formulation has also been shown to improve cardiac function by decreasing the expression of hypertrophic marker genes and apoptotic mediators.
Some curcumin nanoformulations, such as hyaluronic acid-based nanocapsules, nanoparticles encapsulated in PLGA or nanoemulsion systems, have been found to increase the aqueous solubility of curcumin and subsequently prevent hypertension in animals. Similar cardioprotective effects have been observed using nanocurcumin polymer-based nanoparticles, curcumin- and nisin-based polylactic acid nanoparticles. These preparations have been shown to prevent myocardial damage and improve myocardial function.
Effects of curcumin nanoformulation on the brain
Curcumin complexed with galactomannan has been shown to be highly effective in improving blood-brain barrier permeability and preventing neuroinflammation, anxiety, fatigue, and memory loss in both humans and animals.
Liposomes containing curcumin have been shown to exert anti-amyloidogenic and anti-inflammatory effects in animal and cellular models of Alzheimer's disease. Curcumin's preventive effects on Alzheimer's disease are associated with its ability to reduce amyloid-beta production and tau aggregation, which are the main hallmarks of Alzheimer's disease.
However, clinical trials in patients with mild to moderate Alzheimer's disease did not find beneficial effects of curcumin in reducing disease biomarkers and improving cognitive function.
Meanwhile, a recent clinical trial in adults without dementia showed that oral curcumin treatment may improve memory and reduce amyloid and tau accumulation in the amygdala and hypothalamus.
