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.
In the present research work, the motto was to develop new chemical entities as potential anti-inflammatory, analgesic and antipyretic agents. Various 4-(2-amino-6-(substituted)pyrimidin-4-yl)-3-methyl-1-(substituted)-1H-pyrazol-5(4H)-one derivatives (5a-5j) and their Schiff bases (6a-6j) were synthesized. The newly synthesized compounds were characterized by TLC and spectral data. The compounds containing pyrazolone and amino pyrimidine as basic moieties (5a-5j), were screened for their anti-inflammatory, analgesic and antipyretic activities, compounds 5a, 5c-5f, 5h exhibited activities nearly similar to the standard. The pharmacological studies reveal that the presence of 4-hydroxy, 4-methoxy, 4-(N,N-dimethylamino) or 2-hydroxy groups on phenyl ring at C6 of amino pyrimidine exhibits anti-inflammatory, analgesic and antipyretic activities nearly similar to the standard and substitutions like 4-chloro, 2-nitro, 3-nitro or 4-nitro on same phenyl ring lead to a decrease in activities.
The objective of the present study was to develop double layered tablets of lornoxicam, a highly potent nonsteroidal anti-inflammatory drug. Double layered tablets compris of fast release layer and a sustained release layer, anticipating the rapid drug release that starts in the stomach rapidly alleviate the symptoms and continuous in the intestine to maintain the prolonged analgesic effect. Double layered tablets are characterized by initial drug release in the stomach and comply the requirements of sustained release portion of the dosage form. An inclusion complex of lornoxicam with β-cyclodextrin at 1:2 (drug: β-CD) molar ratio, was incorporated in the fast release layer to increase the release rate of lornoxicam in the stomach to produce rapid analgesic effect. Hydroxy propyl methyl cellulose (HPMC), a hydrophilic matrix forming agent, was integrated in the sustained release layer to provide the sustainment of drug release, F2 was selected as the best formulation as it fulfilled all the criteria. The drug release of F2 extended up to 12 h period. Based on the statistical analysis the drug release follows Anomalous diffusion mechanism. Two months of short term stability study were carried out at 30 ± 2°C / 65 ± 5% RH and 40 ± 2°C / 75 ± 5% RH for the best selected formulation. The results showed that there were no significant changes in all the parameters evaluated for the best formulation.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.