In practical applications, curcumin has certain defects, such as low solubility, poor stability, low absorption rate, and easy conversion into glucuronide and sulfonic acid complexes in the intestine, with fast metabolism and short half-life. Its presence has led to its low bioavailability, limiting its use in the food and pharmaceutical industries. As found in human experiments, it can only be detected when the oral dose reaches 10~12 g. Rats are given a dose of 10 mg/kg of curcumin intravenously. The maximum concentration in serum is only 0.36 μg/mL; oral 1.0 g/ After 15 min of kg curcumin, the concentration in rat plasma was only 0.13 μg/mL, and reached the maximum concentration of 0.22 μg/mL after 1 h. After 6 h, the plasma could not be detected. Curcumin was orally administered to rats. Only a small amount was detected in blood, liver and kidney. 90% was found in the stomach and small intestine. After 24 hours, only 1% remained. After intraperitoneal injection of 0.1 g/kg curcumin for 1 h, turmeric was found. The distribution in the organ is very different, with the largest number in the intestine (117 μg / g), second in the kidney, blood and liver, and very low in the brain (0.4 μg / g). Therefore, improving the bioavailability of curcumin will be an important direction worth studying in the future.
The main ways to improve the bioavailability of curcumin are:
(1) Use with appropriate pharmaceutical excipients
For example, if curcumin is combined with hepatic and intestinal glucuronic acid-binding inhibitor piperine, curcumin can be made into a metal ion-containing chelate, such as copper curcumin, to improve its ability to scavenge reactive oxygen species. And pharmacological activity and reduce the toxicity of metal ions.
(2) Synthetic curcumin analogues
The biological activity of curcumin depends to a large extent on its chemical structure. Modification of its benzene ring, methylene and carbonyl groups, and the screening of derivatives and analogues are important ways to improve its bioavailability.
(3) Change product dosage form
At present, the main product formulations of curcumin include solid dispersions, nanoparticles, liposomes, micelles and the like. For example, polyvinylpyrrolidone (PVP) and polyethylene glycol (PEG) are used as carriers to prepare a solid dispersion of curcumin. As a result, the bioavailability of curcumin-PVP solid dispersion in rats is improved compared with ordinary tablets. 590%.
Nano-curcumin has the advantages of long cycle time, strong permeability and resistance to body metabolism, but there are leakage problems. There are a large number of voids between the hydrogel magnetic nanomixtures (HGMNC), and the curcumin molecules can be attached to the surface of the nanoparticles to provide sustained and efficient release. Using HGMNC's sensitivity to external magnetic field stimuli, curcumin can be transported to target sites such as cancer cells to act as a target for disease treatment. The liposome can fuse with the cell membrane, and the curcumin can be sent into the interior of the cell, so that the drug is mainly distributed in tissues and organs such as liver, spleen, lung and bone marrow. However, as a carrier, liposomes have problems such as poor stability and easy leakage.
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