(Difference in the delivery mechanism of free curcumin and nanocurcumin (Source))
First time Wahlstrom and Blennow in 1978 reported that after oral administration of 1 g/kg of curcumin in Sprague-Dawley rats, negligible amounts of curcumin in blood plasma of rats was observed which could be due to its poor absorption from the gut. Later several studies conducted on bioavailability of curcumin found that certain amount of curcumin are bioavailable in the serum of animals. In a study, when curcumin was given orally at a dose of 2 g/kg to rats, a maximum serum concentration of 1.35±0.23 µg/mL was observed at 0.83 hours, whereas in humans the same dose of curcumin resulted in either undetectable or extremely low (0.006±0.005 µg/mL) serum levels after 1 hour [1].
For lipophilic drugs like curcumin, despite their biocompatibility, uptake and retention when administered in-vitro or in-vivo severely impacted their potential. It was identified that curcumin was readily metabolized extensively by the liver and plasma and is reduced or functionalized to tetrahydrocurcumin or hexahydrocurcumin in rats. Curcumin is broken down into its water-soluble metabolites and excreted out of the system through urine. Furthermore, extensive investigation of the pharmacokinetic properties using mouse models were conducted wherein, an hour post administration, the highest accumulation of curcumin was identified in the serum and intestine while trace amounts were detected in the liver, spleen, kidney, and brain respectively [2].
(Comparative overview of the bioavailability of native curcumin vs nanoformulations after 2 hours in cellular assays (Source))
By encapsulating the drug within their tiny structures, nanoparticles can significantly enhance their bioavailability and solubility. While previous efforts to improve curcumin's bio-distribution had limited success, the advent of nanotechnology delivery systems has unlocked its full therapeutic potential. Using physiochemical properties of the delivery systems, the therapeutic effects of curcumin can be utilized to its full potential. This paves the way for exciting new treatment options in various diseases, making nanotechnology a critical driver in the future of medicine.
References:
Ireson, C. et al. Characterization of Metabolites of the Chemopreventive Agent Curcumin in Human and Rat Hepatocytes and in the Rat in Vivo, and Evaluation of Their Ability to Inhibit Phorbol Ester-induced Prostaglandin E2 Production1. Cancer Res 61, 1058–1064 (2001).
El-Saadony Mohamed T., Yang Tao, Korma Sameh A., Sitohy Mahmoud et. al., Impacts of turmeric and its principal bioactive curcumin on human health: Pharmaceutical, medicinal, and food applications: A comprehensive review. Front. Nutr., 10 January 2023. Sec. Nutrition and Metabolism, Volume 9 - 2022, https://doi.org/10.3389/fnut.2022.1040259
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