Enhanced Water Dispersibility of Curcumin Encapsulated in Alginate-Polysorbate 80 Nano Particles and Bioavailability in Healthy Human Volunteers.

BACKGROUND: The turmeric (Curcuma longa) plant, a perennial herb of the ginger family, is an agronomic crop in the south and southeast tropical Asia. Turmeric an Indian yellow gold and universal spice is described in Ayurveda, an ancient treatise on longevity and quality life for the treatment of various inflammatory disorders. The oral bioavailability of curcumin is low due to poor aqueous solubility, alkaline instability and speedy elimination. OBJECTIVE: The present study is designed to prepare alginate polysorbate 80 nanoparticles to enhance aqueous solubility/dispersibility, hence bioavailability. METHOD: Curcumin-loaded alginate - polysorbate 80 nanoparticles were prepared by ionotropic gelation technique. RESULTS: The optimized nano particles exhibited higher encapsulation efficiency (95%), particle size of 383 nm and Zeta potential of +200 mV. Formulations exhibited very low dissolution in Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF), but the major portion released in SCF which is attributed to the digestibility of alginate in Simulated Colonic Fluid (SCF) under the influence of colonic micro flora. FTIR and DSC observations revealed the successful entrapment of curcumin in alginate polysorbate-80 nanoparticles. The nanoparticles were more spherical, discrete and homogeneous. In healthy human volunteers, the oral bioavailability (AUC) of curcumin increased 5-fold after the consumption of curcumin nanosuspension compared to curcumin suspension. Maximum plasma concentration Cmax- 636 ± 122 ng/ml was observed at tmax- 2h for nanosuspension, whereas Cmax-87.7 ± 17.9ng/ml at tmax- 4h for suspension. CONCLUSION: Curcumin-loaded alginate - polysorbate 80 nanoparticles prepared by ionotropic gelation method, successfully entrapped curcumin. Both curcumin suspension and curcumin nanosuspension were safe and well tolerated and may thus be useful in the prevention or treatment of various inflammatory diseases of mankind.

Synthesis pharmacological evaluation and docking studies of pyrimidine derivatives.

A new group of pyrimidine derivatives of indane-1,3-dione were synthesized aiming at the synthesis of new compounds acting as analgesic, anti-inflammatory and antimicrobial activity in a single component. The title compounds (3a-l) were synthesized from chalcone derivatives of indane-1,3-dione (2a-l) through cyclization reaction with urea. The synthesized compounds were characterized by FT-IR, (1)H NMR, mass spectral data, elemental analysis and evaluated for anti-inflammatory, analgesic, antibacterial and antifungal activities. The most active compound 3e, was evaluated for its ulcerogenicity. Good anti-inflammatory property was observed for chlorophenyl substituted pyrimidine derivatives. It mainly binds with Pro 218 of 1CX2, and the ligand could have caused much conformational changes in the protein structure than other derivatives. It also exhibits good analgesic and antimicrobial agent in a single component.

Protective effect of the hydro-alcoholic extract of Rubia cordifolia roots against ethylene glycol induced urolithiasis in rats.

UNLABELLED: This study investigated the protective effect of the hydro-alcoholic extract of roots of Rubia cordifolia Linn. (HARC) against ethylene glycol induced urolithiasis and its possible underlying mechanisms using male Wistar albino rats. Ethylene glycol feeding resulted in hyperoxaluria, hypocalciuria as well as increased renal excretion of phosphate. Supplementation with HARC significantly prevented change in urinary calcium, oxalate and phosphate excretion dose-dependently. The increased calcium and oxalate levels and number of calcium oxalate crystals deposits in the kidney tissue of calculogenic rats were significantly reverted by HARC treatment. The HARC supplementation also prevents the impairment of renal functions. RESULTS: Indicate that the HARC can protect against ethylene glycol induced urolithiasis as it reduced and prevented the growth of urinary stones. Therefore, HARC is helpful to prevent the recurrence of the disease as it showed its effect on early stages of stone development. The mechanism underlying this effect is mediated possibly through an antioxidant, nephroprotection and its effect on the urinary concentration of stone-forming constituents and risk factors.

In vivo rodent micronucleus assay of gmelina arborea roxb (gambhari) extract.

Gmelina arborea Roxb (family Verbenaceae) commonly known as 'Gambhari' tree, the various parts of the plants are widely used in diarrhoea, anti-pyretic, thirst, anemia, leprosy, ulcers, consumption, strangury, vaginal discharges. We tested the genotoxic potential of G. arborea in bone marrow cells obtained from Swiss albino mice using micronuclei formation as the toxicological endpoints. Aqueous extract of G. arborea (AEGA) was tested at the dose of 286 & 667 mg/kg body weight (b. w.). Cyclophosphamide (CPZ) 25 mg/kg b. w. was used as positive control in micronucleus test. The AEGA significantly increased the % micronucleated polychrometics at doses of 286mg/kg and 667mg/kg, after 24, 48 72h time interval. And also decreased the PCE/NCE ratio after 24, 48 and 72 h as compared to solvent control group. In this study, we investigated the effect of G. arborea on mammalian bone marrow cells using micronuclei formation to assess the genotoxicity of the herb.