Recent advances to improve curcumin oral bioavailability

Sabet, Saman; Rashidinejad, Ali; Melton, Laurence D.; McGillivray, Duncan J.

doi:10.1016/j.tifs.2021.02.006

Cited by 92 publications

(49 citation statements)

References 107 publications

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“…On the other hand, several studies have indicated a significant intrinsic activity and, hence, efficacy of curcumin as a therapeutic molecule for different conditions. Nevertheless, studies over the past few decades related to ADME of curcumin have demonstrated limited absorption and rapid metabolism of curcumin that markedly limits its bioavailability [37]. For instance, peroral administration of a higher dose of curcumin in rats (500 mg/kg) produced the C max value of 60 ng/mL [38] and bioavailability of 1%, which is substantially lower than the C max value (110.45 ng/mL) and bioavailability (~ 5%) of HZC observed in the current study at a dose of 100 mg/kg.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats

Satyavert¹,

Gupta²,

Choudhury

et al. 2021

Pharmacol. Rep

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Background Curcumin, a natural polyphenol from Curcuma longa, is known to possess diversified pharmacological roles including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic properties; however, its bioavailability is severely limited due to its poor solubility, poor absorption, rapid metabolism, and significant elimination. Hydrazinocurcumin (HZC), a novel analogue of curcumin has been reported to overcome the limitations of curcumin and also possesses multiple pharmacological activities. The present study aimed to evaluate the unexplored pharmacokinetic profile of this agent in experimental rats. Methods Drug formulations were administered to the experimental animals via oral, intravenous and intraperitoneal routes. Blood samples were collected at different pre-determined time intervals to determine the pharmacokinetic parameters. To understand the biodistribution profile of HCZ, tissue samples were isolated from different groups of Sprague-Dawley rats at different time points. The pharmacokinetic parameters of HZC were evaluated after administration through oral (100 mg/ kg), intraperitoneal (100 mg/kg) and intravenous (10 mg/kg) routes. Results Significantly (p < 0.05) higher total AUC along with maximum concentration were evident with intraperitoneal administration when compared to the results of oral administration at a similar dose. In addition, shorter time to peak was observed with intraperitoneal administration. These results revealed a faster rate and longer duration of absorption with intraperitoneal administration, which further resulted in enhanced absolute bioavailability of HZC (29.17%) when compared to 5.1% upon oral dosing. The obtained data from the pharmacokinetic study indicated that HZC was instantaneously distributed and moderately eliminated from body fluids. Conclusion Based on the findings, it could be concluded that absorption of HZC is much higher via intraperitoneal route of administration compared to the oral administration.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats

Satyavert¹,

Gupta²,

Choudhury

et al. 2021

Pharmacol. Rep

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“…In contrast, at alkaline pH (pH > 8), log P of Cur decreases and reaches −3.4 at pH 14, rendering it readily soluble in water. However, its half-life was significantly shortened to around 2.1 min at pH 7.98 (Kharat & McClements, 2019;Sabet et al, 2021). Hence, stability of Cur is much lower at neutral and alkaline pH than at acidic pH.…”

Section: Curcuminmentioning

confidence: 98%

“…Apart from sensitivity to neutral and alkaline pH, Cur is also susceptible to thermal, oxidative, and photo-degradation (higher rate under visible than UV light) (Kharat & McClements, 2019). However, it has been reported that Cur is much more stable in oil than in water, and the encapsulation of Cur within oil droplets appeared to improve its physicochemical stability (Kharat et al, 2017;Sabet et al, 2021).…”

Section: Curcuminmentioning

confidence: 99%

Advances in smart delivery of food bioactive compounds using stimuli‐responsive carriers: Responsive mechanism, contemporary challenges, and prospects

Shishir

Gowd

Suo

et al. 2021

Comp Rev Food Sci Food Safe

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Many important food bioactive compounds are plant secondary metabolites that have traditional applications for health promotion and disease prevention. However, the chemical instability and poor bioavailability of these compounds represent major challenges to researchers. In the last decade, therefore, major impetus has been given for the research and development of advanced carrier systems for the delivery of natural bioactive molecules. Among them, stimuli-responsive carriers hold great promise for simultaneously improving stability, bioavailability, and more importantly delivery and on-demand release of intact bioactive phytochemicals to target sites in response to certain stimuli or combination of them (e.g., pH, temperature, oxidant, enzyme, and irradiation) that would eventually enhance therapeutic outcomes and reduce side effects. Hybrid formulations (e.g., inorganic-organic complexes) and multi-stimuli-responsive formulations have demonstrated great potential for future studies. Therefore, this review systematically compiles and assesses the recent advances on the smart delivery of food bioactive compounds, particularly quercetin, curcumin, and resveratrol through stimuli-responsive carriers, and critically reviews their functionality, underlying triggered-release mechanism, and therapeutic potential. Finally, major limitations, contemporary challenges, and possible solutions/future research directions are highlighted. Much more research is needed to optimize the processing parameters of existing formulations and to develop novel ones for lead food bioactive compounds to facilitate their food and nutraceutical applications.

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“…Despite numerous health benefits, curcumin’s limited bioavailability is a fundamental criticism [ 10 ]. Low absorption, fast metabolism, chemical instability, and rapid systemic clearance have been suggested as possible causes [ 11 ].…”

Section: Bioavailability Of Curcuminmentioning

confidence: 99%

The Multifaceted Role of Curcumin in Advanced Nanocurcumin Form in the Treatment and Management of Chronic Disorders

Tagde

Tagde²,

Islam

et al. 2021

Molecules

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Curcumin is the primary polyphenol in turmeric’s curcuminoid class. It has a wide range of therapeutic applications, such as anti-inflammatory, antioxidant, antidiabetic, hepatoprotective, antibacterial, and anticancer effects against various cancers, but has poor solubility and low bioavailability. Objective: To improve curcumin’s bioavailability, plasma concentration, and cellular permeability processes. The nanocurcumin approach over curcumin has been proven appropriate for encapsulating or loading curcumin (nanocurcumin) to increase its therapeutic potential. Conclusion: Though incorporating curcumin into nanocurcumin form may be a viable method for overcoming its intrinsic limitations, and there are reasonable concerns regarding its toxicological safety once it enters biological pathways. This review article mainly highlights the therapeutic benefits of nanocurcumin over curcumin.

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Recent advances to improve curcumin oral bioavailability

Cited by 92 publications

References 107 publications

Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats

Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats

Advances in smart delivery of food bioactive compounds using stimuli‐responsive carriers: Responsive mechanism, contemporary challenges, and prospects

The Multifaceted Role of Curcumin in Advanced Nanocurcumin Form in the Treatment and Management of Chronic Disorders

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