Pharmacokinetic Profile of Curcumin and Nanocurcumin in Plasma, Ovary, and Other Tissues

Abstract

Background Curcumin is a natural diphenolic compound that is currently being investigated for various cancers, including ovarian cancer. Clinical application of curcumin has been limited due to its low solubility and bioavailability and rapid metabolism and degradation at physiological pH. Particle size is one factor that can affect the absorption process, which thus increases compound solubility and transport across the membrane. This study was conducted to determine the effects of modifying the particle size of curcumin on its pharmacokinetic parameters in blood and other organs. Methods Female Sprague Dawley rats were administered a single oral dose of 500 mg/kg curcumin or nanocurcumin. Blood samples were collected at 10, 15, 30, 45, 75, and 120 min, and ovaries, livers, kidneys, and colons were collected at 180 min. The levels of curcumin in plasma and organs were determined using UPLC-MS/MS, and the pharmacokinetic parameters were evaluated. Results Curcumin levels were detectable and measurable in plasma and organs of rats that were administered curcumin or nanocurcumin. Overall, no statistically significant differences were found in pharmacokinetic parameters between curcumin and nanocurcumin groups in both plasma and organs, except for ovaries. The curcumin levels in plasma, liver, kidney, and colon in the curcumin group were higher than those in the nanocurcumin group. However, curcumin concentrations in ovaries in the nanocurcumin group were 3.6 times higher than those in the curcumin group. Conclusion Particle size reduction of curcumin did not increase the concentration of curcumin in the plasma but increased its distribution in the ovaries.

Pharmacokinetics and Pharmacodynamics of the Combination of Rhein and Curcumin in the Treatment of Chronic Kidney Disease in Rats

“…In this study, the concentration of curcumin in renal tissue was determined at three different periods including 30 min, 1 h, 2 h after administration. The measured concentration of curcumin in renal tissue was very low when administrated on its own, which was consistent with the literatures ( Gutierres et al, 2015 ; Arozal et al, 2019 ). However, after combination with rhein, the level of curcumin in renal tissue was nearly doubled in 30 min after administration.…”

“…The concentration of rhein in renal tissue was increased more than 2-fold after co-administration (2.62 ± 0.70 μg/ml vs. 7.00 ± 0.65 μg/ml), indicating that combination with curcumin promoted the affinity of rhein with renal tissue. A previous study on the tissue distribution of curcumin showed that the concentration of curcumin in the heart, liver and kidney was extremely low ( Gutierres et al, 2015 ; Arozal et al, 2019 ). In this study, the concentration of curcumin in renal tissue was determined at three different periods including 30 min, 1 h, 2 h after administration.…”

Development, Characterization and Pharmacokinetic Profile of Chitosan-Sodium Tripolyphosphate Nanoparticles Based Drug Delivery Systems for Curcumin

“…The calibration curve of a standard solution was made with the final level of the analytes at 1, 2.5, 5, 10, 25, and 50 ng/mL. 24 The pharmacokinetic profiles were represented as mean and standard error (SE) from each group and were estimated through non-compartmental analysis. Pharmacokinetic parameters are calculated based on the curcumin concentration curve in plasma versus time.…”

Construction a Long-Circulating Delivery System of Liposomal Curcumin by Coating Albumin

“…In addition, curcumin is stabilized in a solution with a pH < 6.5, and the degradation rate is significantly accelerated as the pH value of the solution increased. These properties of curcumin seriously limit its clinical application. − As we know, liposomes have shown great potentials in drug delivery due to its drug-loading capacity, avoiding immune response, biodegradability, and biocompatibility. − Liposomes are composed of a hydrophobic lipid bilayer and a hydrophilic inner aqueous chamber; lipophilic drugs can distribute in lipid bilayers in high percentages. − Therefore, the liposomes as the carrier of curcumin have obvious advantages and several recent studies have confirmed this. − Our previous study also found that the water-solubility and stability of curcumin were significantly improved after encapsulating it into liposomes …”

“…These properties of curcumin seriously limit its clinical application. 6 − 9 As we know, liposomes have shown great potentials in drug delivery due to its drug-loading capacity, avoiding immune response, biodegradability, and biocompatibility. 10 − 12 Liposomes are composed of a hydrophobic lipid bilayer and a hydrophilic inner aqueous chamber; lipophilic drugs can distribute in lipid bilayers in high percentages.…”