An open label, balanced, randomized, parallel, single dose, comparative bioavailability study of four different Curcumin formulations (containing Curcumin 600mg) of Sanat Products Ltd., India in 20 Healthy adult human male subjects under fasting conditions.

BackgroundTurmeric, the source of the polyphenolic active compound curcumin (diferuloylmethane), has been used extensively in traditional medicine since ancient times as a household remedy against various diseases, including hepatic disorders, cough, sinusitis, rheumatism, and biliary disorders. Recently a large number of studies have shown that curcumin (CU) has a surprising array of antioxidant, antitumor, anti-inflammatory, anticancer, and other desirable medicinal properties.

There is scientific evidence suggesting that CU has a highly pleotropic structure, that physically interacts with a wide range of molecular targets, e.g., transcription factors, growth factors and their receptors, cytokines, enzymes, and genes regulating cell proliferation. Curcumin (CU) functions as an anti-cancer agent by activating apoptosis signaling and inhibiting cell proliferation. CU has been shown to suppress the expression of epidermal growth receptor and estrogen receptors, which are cancer-associated growth factors (Duvoix et al., 2003; Tapal and Tiku, 2012).

However, the main drawback associated with CU is its poor aqueous solubility (11 ng/mL) (Kaminaga et al., 2003), stability in gastrointestinal fluids, low permeability and first pass metabolism which leads to poor bioavailability (~1% in rat) (Pan et al., 1999; Yang et al., 2007). CU is a BCS Class IV (low solubility low permeability) molecule (Wahlang et al., 2011). In order to deliver CU to targeted organs, its hydrophobic property needs to be modified. The small size of carriers is very important for the biodistribution in the body. The capillaries are so small that red blood cells can only travel through them in single file. The capillaries measure approximately 5–10 μm in diameter. Particles larger than this size cannot be circulated in the body and become entrapped in the capillary bed. Thus, the particle diameter should be generally smaller than micrometers for the particles to be circulated in the blood vessels. In addition, reduction in the particle diameter to less than 100 nm is thought to decrease their removal by  thereticuloendothelial system and increase their extravasations from the smallest capillaries. Thus, nanotechnology is one of the effective methods to be used for the delivery of CU.

  Study Rationale:The rational for the present study was to increase the bioavailability of Curcumin for increasing the therapeutic effectiveness against different ailments using Nano particle size of Curcumin in tablet form through oral route as the drug delivery approach.

The study has been designed to augment the in vitro release by improving solubility and permeability using Curcumin Nanoparticles and to enhance the bioavailability of Curcumin by delivering it at the molecular level in the form of nano particles.