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Bioavailable curcumin

Curcumin has a low bioavailability.

Traditional uses and properties of curcumin

Curcumin is a natural polyphenol extracted from the dried rhizomes of turmeric (Curcuma longa L.). It is a gold-coloured spice traditionally used the Indian subcontinent for health care, food conservation and as a dye for textiles.

 

Curcumin has been used for centuries in its originating countries to treat numerous illnesses, including rheumatism, body ache, skin diseases, digestive and inflammatory disorders,... Over the last few years, a number of studies have reported evidence of several pharmacological properties of curcumin, including anti-inflammatory and immunomodulatory effects.

 

Bioavailability of curcumin 

However, the potential use of curcumin in chemopreventive or therapeutic settings has been hindered by its low bioavailability after oral administration.  In consequence, new formulations are needed to enhance it as well as more extensive and well-controlled clinical trials to fully evaluate its potential in terms of optimal use.

bioXtract has developed an innovative formulation for a more bioavailable curcumin. This formulation has proven its efficacy on humans.

 

 

Osteoarthritis Efficacy: In vitro Trials

Curcumin is used in our alternative therapy for osteoarthritis sufferers, Artiflex.The activity and efficacy of Artiflex active principle (curcumin) have been evaluated by the “Bone and Cartilage Research Unit” in the Liege Hospital (Belgium), under the Direction of Prof. Henrotin.

 

BCRU is highly specialized in the pre-clinical and clinical investigation of drugs used in the treatment of bone and joint diseases. BCRU has an extensive expertise in the study of the pathophysiological events involved in osteoporosis and osteoarthritis, mainly in the study of the biochemical factors involved in cartilage degradation and senescence. BCRU has developed elegant methods for studying cytokines network, oxidative stress, cartilage matrix repair and degradation and bone remodelling.

 

Curcumin activity and efficacy have been evaluated on three models, rigorously selected as predicting models for efficacy in humans:

 

  • Chondrocytes (bovines and humans) metabolism in basal conditions or IL1b stimulated,
  • Matrix formation model (human chondrocytes in alginate beads),
  • Human cartilage explants.

The results of this study have been published in Inflammation Research (Mathy-Hartert M, Jacquemond-Collet I, Priem F, Sanchez C, Lambert C, Henrotin Y. Curcumin inhibits pro-inflammatory mediators and metalloproteinase-3 production by chondrocytes. Inflamm. Res. 2009; 58: 899-908).

 

This in vitro study demonstrated that :

 

  • Curcumin is an inhibitor of pro-inflammatory mediators: PGE2, IL-6 and IL-8,
  • Curcumin inhibits Cox-2, but not Cox-1 gene expression,
  • In contrast to conventional NSAIDs, curcumin inhibits the synthesis of NO,
  • Curcumin decreases the MMP-3 / TIMP-1 ratio by inhibiting MMP-3 synthesis,
  • Curcumin antagonizes the stimulating effects of IL-1b on the synthesis of PGE2, NO, IL-6, IL-8 and MMP-3.
Bioavailable curcumin has anti inflammatory properties.
PGE2 inhibition by curcumin (Human cartilage explants)

 

 

Curcumin as Immunomodulator

 

 

Curcumin comes from turmeric in a low bioavailable form.

Turmeric has been used in Asian countries particularly in ancient Indian medicine for allergy and asthma treatment.

Curcumin is, along with quercetin, used in Nasaler, the remedy developed by bioXtract as a natural treatment for allergic rhinitis.

 

Anti-allergy properties

Curcumin was reported to have anti-allergic properties with inhibitory effect on histamine release from mast cells. The effectiveness of curcumin in allergy and asthma has been further investigated using a murine model of allergy.

 

The results indicate a marked inhibition of allergic response in animals treated with curcumin suggesting a major role for curcumin in reducing the allergic response. It can thus be used to prevent and cure allergic rhinitis.

 

Immunomodulator effect

Curcumin also has capabilities to modulate the activation of T cells, macrophages, neutrophils, natural killer (NK) cells, and dentritic cells, downregulate various proinflammatory cytokines and chemokines, and enhance anitbody responses.

 

Curcumin presents a large-spectrum anti-inflammatory activity, allowing it to act on different cell populations and then to treat the long term symptoms of rhinitis even in the chronic phase.

 

Bibliographical data show that curcumin presents a corticosteroid activity on different models of allergy (murine model of specific and non specific allergy). In humans, clinical studies have demonstrated the corticosteroid activity of curcumin on other pathologies than allergy, but involving the same inflammatory factors.

 

On top of these proven corticosteroid activities, curcumin is active on neutrophils and on histone desacetylase, which is not the case with corticosteroids.

 

 

Bioavailable curcumin

Curcumin is highly lipophilic and almost insoluble in water at pH values below 7. The solubility is a critical parameter when it comes to bioavailability of curcumin as a potential drug. The low aqueous solubility is probably the most important factor contributing to the low absorption of curcumin from the gastrointestinal tract and the low bioavailablity previously reported [1].

 

bioXtract has developed an innovative proprietary formulation to enhance the solubility of this active principal, using β-cyclodextrin complexation, as well as other highly solubilising additives.

 

Bioavailability of bioXtract innovative curcumin formulation has been evaluated on humans, showing higher plasma levels of active principal compared to standard curcumin formulations.

 


[1] Hegge AB, Schüller RB, Kristensen S, Tonnesen HH. In vitro release of curcumin from vehicles containing alginate and cyclodextrin. Studies of curcumin and curcuminoids. XXXIII. Pharmazie. 2008; 63: 585-592.