A overview article revealed within the journal Antioxidants supplies an in depth overview of nanoparticle-based methods to enhance the bioavailability and bioactivity of curcumin.
Examine: Enhancing the Bioavailability and Bioactivity of Curcumin for Illness Prevention and Therapy. Picture Credit score: Microgen / Shutterstock
Background
Curcumin, turmeric’s essential bioactive compound, is a polyphenol present in Curcuma longa roots. This compound has quite a few well being advantages, together with anticancer, antioxidant, anti-inflammatory, anti-obesity, anti-diabetic, anti-microbial, wound-healing, and lipid-lowering properties.
Curcumin has low bioavailability in human organs and is quickly transformed to a variety of bioactive metabolites after intestinal absorption. Dried turmeric powder ready from Curcuma longa roots accommodates about 2-5% of curcumin.
Curcumin consumed by dietary sources is ample to impression the intestine microbiota. Nevertheless, as a result of fast metabolism, the focus of intact curcumin within the circulation turns into very low (sub-micromolar concentrations), which is inadequate to set off mobile signaling and gene expression, as noticed in in vitro research with cultured cells.
Examples of curcumin nano-delivery programs.
Methods to extend curcumin bioavailability
Dietary curcumin is inefficiently absorbed throughout the intestinal epithelium and undergoes fast metabolism and systemic elimination. In an aqueous answer with a impartial pH, the enol state of curcumin is fashioned, which reduces the soundness of curcumin.
A number of nanoformulations have been developed to extend curcumin focus within the circulation in addition to in particular cells, tissues, and organelles. These nanoformulations have been designed to extend curcumin solubility, enhance stability throughout gastrointestinal absorption, alter absorption routes, and inhibit cleansing enzymes utilizing adjuvants.
The newest technology of curcumin nanoformulations can improve free curcumin bioavailability in plasma by greater than 100-fold and enhance absorption, mobile uptake, permeability by the blood-brain barrier, and tissue distribution.
Elements that enhance curcumin bioavailability embody composition, dimension, and route of administration of nanoparticles. Curcumin preparations with smaller-size nanoparticles have been discovered to extend bioavailability when administered orally. In distinction, larger-size nanoparticles have been discovered to extend bioavailability when administered intravenously.
Curcumin nanoformulations can induce senescence in malignant and regular cells, thus successfully treating numerous most cancers varieties and age-related illnesses, together with cardiometabolic illnesses, neurodegenerative illnesses, and liver, lung, and gastrointestinal illnesses.
Relating to mode of motion, current proof signifies that curcumin acts as an antioxidant and anti inflammatory compound to cut back the manufacturing of reactive oxygen species (ROS) and modulate mobile signaling and gene expression associated to inflammatory pathways. These actions work synergistically to take care of homeostasis of mobile macromolecules (proteins, DNA, and lipids).
These actions could be elevated by incorporating curcumin in nanoparticle-based formulations, corresponding to polymeric curcumin–bioperine–PLGA. The isomerization of curcumin to cis-trans curcumin is thought to extend its skill to bind adenosine receptors. Incorporation of cis-trans curcumin into nanoformulations is taken into account to be a worthwhile technique to extend its therapeutic efficacy in opposition to inflammatory illnesses.
Relating to security profile, current scientific trials point out that almost all of curcumin nanoformulations are well-tolerated and secure to be used in people.
Anti-microbial actions
Curcumin is thought to exert an anti-microbial impact in opposition to each Gram-positive and Gram-negative micro organism, and this exercise is helpful for topical purposes in opposition to pores and skin an infection and oral and intestinal purposes. Furthermore, curcumin can not directly forestall an infection by inhibiting bacterial progress in meals.
The anti-microbial actions of curcumin could be enhanced by incorporating it into nanoformulations. Administration of curcumin with different compounds, corresponding to antibiotics, honey, or different polyphenols, may also improve its anti-microbial and biofilm inhibitory actions.
Results of curcumin nanoformulations within the gastrointestinal tract
A number of nanotechnology-based programs, corresponding to micelles, liposomes, exosomes, phospholipid complexes, nanoemulsions, nanostructured lipid carriers, and biopolymer nanoparticles, have been discovered to extend oral curcumin bioavailability.
Nanoparticle curcumin referred to as ‘Theracurmin’ has been discovered to suppress colitis in mice by modulating intestine microbiota. Enchancment in intestine microbiota composition has additionally been achieved utilizing nanobubble curcumin extract. Curcumin loaded with nanostructured lipid carriers has been discovered to cut back colonic irritation in animals.
The incorporation of curcumin in liposomes has been discovered to extend its anticancer exercise by enhancing gastrointestinal absorption. Furthermore, the administration of curcumin with different bioactive compounds, corresponding to piperine and salsalate, has been discovered to extend curcumin bioavailability and bioactivity.
Results of curcumin nanoformulations in liver and adipose tissue
Curcumin nanoformulations with adjuvants, corresponding to piperine and quercetin, have been discovered to extend its bioavailability and bioactivity considerably. Numerous nanotechnology-based supply programs, corresponding to micelles, liposomes, polymeric, metallic, and strong lipid nanoparticles, have been discovered to extend curcumin bioavailability.
The anti-inflammatory, antioxidant, and antifibrotic properties of curcumin make it a possible therapeutic compound for liver illnesses. In liver illnesses, curcumin nanoformulations have been discovered to extend its therapeutic efficacy by growing curcumin solubility, bioavailability, and membrane permeability and enhancing its pharmacokinetics, pharmacodynamics, and biodistribution.
Results of curcumin nanoformulations on the cardiovascular system
Curcumin encapsulated in carboxymethyl chitosan nanoparticles conjugated to a myocyte-specific homing peptide has been discovered to extend the cardiac bioavailability of curcumin. The formulation has additionally been discovered to enhance cardiac perform by lowering the expression of hypertrophy marker genes and apoptotic mediators.
A number of curcumin nanoformulations, corresponding to hyaluronic acid-based nanocapsules, nanoparticles encapsulated in PLGA or nanoemulsion programs, have been discovered to extend the aqueous solubility of curcumin and subsequently forestall hypertension in animals. Comparable cardio-protective results have been noticed utilizing nanocurcumin polymer-based nanoparticles and curcumin and nisin-based polylactic acid nanoparticles. These formulations have been discovered to stop myocardial injury and enhance cardiac muscle capabilities.
Results of curcumin nanoformulations on the mind
Curcumin complexed with galactomannans has been discovered to have higher blood-brain barrier permeability and better efficacy in stopping neuroinflammation, nervousness, fatigue, and reminiscence loss in each people and animals.
Curcumin-laden liposomes have been discovered to exert anti-amyloidogenic and anti inflammatory results in animal and mobile fashions of Alzheimer’s illness. Curcumin’s preventive actions in opposition to Alzheimer’s illness are related to its skill to cut back amyloid-beta manufacturing and tau aggregation, that are main hallmarks of Alzheimer’s illness.
Nevertheless, scientific trials involving sufferers with gentle to reasonable Alzheimer’s illness couldn’t discover any useful impact of curcumin in lowering illness biomarkers and enhancing cognitive capabilities.
A current scientific trial involving non-demented adults, then again, has proven that oral curcumin remedy can enhance reminiscence and scale back amyloid and tau accumulation within the amygdala and hypothalamus.
