Abstract
Objective: The objective of the present work was to improve aqueous solubility and in vivo bioavailability of curcumin and structural analogues of curcumin such as potassium, calcium, magnesium salts and nitro derivative.
 Methods: Structural analogues of curcumin were prepared by reaction of curcumin with potassium chloride, magnesium chloride hexahydrate and calcium chloride dihydrate in a suitable solvent. The nitro derivative synthesized by treating curcumin with sulphuric acid and nitric acid. The prepared analogues were evaluated for melting behavior, solubility, UV spectrophotometry, partition coefficient, moisture content, cellular uptake, FTIR analysis, antimicrobial activity and in vivo bioavailability in the rat.
 Results: Chemical modification of curcumin increased the saturation solubility to 11.6, 16.5, 21.5, 28.0 µg/ml in calcium salt, magnesium salt, potassium salt and nitro derivative respectively, against 8.6 µg/ml of curcumin. The analogues were chemically stable as curcumin analyzed by FTIR spectrophotometry. Increased cellular uptake, as well as enhanced antimicrobial activity, was demonstrated by modified curcumin analogues. Moreover, significant improvement in plasma levels was estimated with nitro derivative.
 Conclusion: The present work recommends that nitration of curcumin improves aqueous solubility which may improve absorption and in vivo bioavailability.
Highlights
Curcumin, a naturally occurring polyphenolic diferuloylmethane extracted from the rhizomes of plant Curcuma longa Linn. (Family: Zingiberaceae) has potential in the prevention and therapeutic interventions of several pathological conditions including respiratory diseases, inflammation, liver disorders and diabetic wounds
Melting points for curcumin and its potassium, magnesium, calcium salts and nitro derivative were found to be in the range of 182-184 °C, 320-325 °C, 310-312 °C, 330-332 °C and 210-220 °C respectively
The enhanced solubility data were supported by UV spectral analysis, partition coefficient determination as well as improved cellular uptake by RBC
Summary
A naturally occurring polyphenolic diferuloylmethane extracted from the rhizomes of plant Curcuma longa Linn. (Family: Zingiberaceae) has potential in the prevention and therapeutic interventions of several pathological conditions including respiratory diseases, inflammation, liver disorders and diabetic wounds. (Family: Zingiberaceae) has potential in the prevention and therapeutic interventions of several pathological conditions including respiratory diseases, inflammation, liver disorders and diabetic wounds. It prevents a variety of carcinogen-induced cancers in rodents by suppressing the mutagenic effects of carcinogens [1]. In spite of its efficacy and safety, curcumin has not yet been approved as a therapeutic agent due to its low bioavailability presenting a significant pharmacological obstacle for clinical application. It is a hydrophobic compound with poor aqueous solubility and low absorption. Many attempts have been made to increase solubility, absorption (permeability) and stability of curcumin in order to increase bioavailability
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