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Complexities of Curcumin Formulations in Body Absorption

Complexities of Curcumin Formulations in Body Absorption

Curcumin is the bioactive constituent isolated from turmeric, which is used for seasoning, pigment, and herbal medicine in food. It has been considered the most common nutraceutical used in pharmaceutical, supplement, and food domains due to its several health benefits. When consumed as a drug, supplement, or food, it consists of antioxidant, anti-inflammatory, antimicrobial, anti-parasite, and anticancer activities. Its toxicity is determined by conducting clinical studies for analyzing its safety in terms of consumption, even at relatively high levels. It’s biological mechanisms, and low toxicity have resulted in an effective nutraceutical ingredient for application in functional foods. But, there are many hurdles that formulators need to mitigate while incorporating curcumin into commercial products. The low water solubility, mainly under acidic and neutral conditions, chemical instability in neutral and alkaline conditions, rapid metabolism by enzymes in the human body, and limited bioavailability are the significant complexities found during formulations of curcumin which brings complexities during absorption in the body. Hence, a minimal amount of curcumin is ingested into the bloodstream. Therefore, there is a need for overcoming such obstacles in the absorption of curcumin within the bloodstream. 

The complexity of curcumin in absorption within the bloodstream

 Pure curcumin is an orange and yellow coloured crystalline material that is available in powdered form. Its chemical composition is considered a labile hydrophobic substance is evolving with low water solubility, mainly under acidic or neutral conditions showing complete protonation. Also, poor chemical stability in alkaline conditions and low bioavailability in case of lower bioaccessibility and chemical transformation due to presence of metabolic enzymes in the gastrointestinal tract contributes to its slower absorption rate. Curcumin is also susceptible to chemical degradation when stored in the body during the condition of light, high temperatures, and alkaline conditions (Tønnesen et al., 2002). During acidic conditions, curcumin shows stability towards chemical degradation while constituting low water solubility that enhances crystallization and sedimentation in aqueous delivery systems (Kharat et al., 2017). Hence, these obstacles complicate the absorption of curcumin within the bloodstream when ingested as pharmaceuticals, supplements, and functional food products. 

Curcumin is lipophilic and contributes to its poor absorption. Most dietary compounds are absorbed within the digestive tract and do not reach the colon. Hence, curcumin concentration in the large intestine can be increased through appropriate ingestion. Poor water solubility is considered a significant issue that hinders the delivery of curcumin to non-enteric organs. The limitations in the solubility and absorption result in lowering the bioactivity of curcumin within non-enteric organs. This complexity is further increased by implicating the understanding that curcumin may not be much effective due to its parent molecule. Still, the effectiveness is determined in some cases due to its metabolites. Most curcumin particles are suggested to get metabolized in the liver and later converted into curcumin conjugates and degradation products (Hoehle et al., 2006). The current inconsistencies in curcumin are due to its lack of stability, short retention time, and limited reports on curcumin’s metabolites and conjugates.

Overcoming curcumin complexities in body absorption

Several approaches have been undertaken for mitigating the complexities of curcumin in terms of absorption. The most effective means of protecting curcumin from chemical degradation is by increasing the water dispersibility and improving its bioavailability through modern encapsulation technologies (McClements et al., 2009). The incorporation of curcumin into edible nanoparticles or microparticles enhances the absorption rate of curcumin, which can be later used to be integrated into food or supplement products (Zhang et al., 2015). The colloidal particles used for the same are assembled from food-grade ingredients involving surfactants, phospholipids, lipids, proteins, polysaccharides, and minerals, using spontaneous or directed processes. Different types of colloidal particles have been used to improve the solubility of curcumin while integrating as micellar aggregates, liposomes, emulsion droplets, solid lipid particles, and biopolymer particles (McClements et al., 2007). 

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References

  1. Tønnesen H.H., Másson M., Loftsson T. Studies of curcumin and curcuminoids. Xxvii. Cyclodextrin complexation: Solubility, chemical and photochemical stability. Int. J. Pharm. 2002;244:127–135.
  2. Kharat M., Du Z., Zhang G., McClements D.J. Physical and chemical stability of curcumin in aqueous solutions and emulsions: Impact of ph, temperature, and molecular environment. J. Agric. Food Chem. 2017;65:1525–1532. doi: 10.1021/acs.jafc.6b04815.
  3. Hoehle, S. I., Pfeiffer, E., Sólyom, A. M., & Metzler, M. (2006). Metabolism of curcuminoids in tissue slices and subcellular fractions from rat liver. Journal of agricultural and food chemistry, 54(3), 756-764. https://doi.org/10.1021/jf058146a
  4. McClements D.J., Decker E.A., Park Y., Weiss J. Structural design principles for delivery of bioactive components in nutraceuticals and functional foods. Crit. Rev. Food Sci. Nutr. 2009;49:577–606. doi: 10.1080/10408390902841529.
  5. Zhang Z., Zhang R., Decker E.A., McClements D.J. Development of food-grade filled hydrogels for oral delivery of lipophilic active ingredients: Ph-triggered release. Food Hydrocoll. 2015;44:345–352. doi: 10.1016/j.foodhyd.2014.10.002.

McClements D., Decker E., Weiss J. Emulsion-based delivery systems for lipophilic bioactive components. J. Food Sci. 2007;72:R109–R124. doi: 10.1111/j.1750-3841.2007.00507.x.

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