SYNTHESIS, SCREENING AND NANOTECHNOLOGY BASED IN VIVO DRUG DELIVERYOF CURCUMIN AND ITS ANALOGUES
Journal Title: Asian J of Pharm Sci & Tech - Year 2012, Vol 2, Issue 2
Abstract
ABSTRACT Curcumin (diferuloyl methane; 1, 7-bis-(4-hydroxy-3-methoxyphenyl)-hepta-1, 6-diene-3, 5-dione) is s a natural yellow orange dye derived from the rhizome of Curcuma longa Linn. It possesses divergent pharmacological activities like anti inflammatory, antioxidant, anticancer, anti HIV, hepatoprotective, and anti diabetic activities etc.Curcumin structural analogues were synthesized and reported to possess same or superior activity compared to the curcumin. Analogues were synthesized using different aromatic substituted aldehydes and they were characterized using spectral data (FTIR, NMR). These compounds were previously screened for hepatoprotective activity. Several of them demonstrated hepatoprotective activity. In this study all the synthesised compounds were screened for anti diabetic activity. From all the six compounds synthesized,compound IIand compound IIIshowed highly significant activity than curcumin and are comparable to standard drug glibenclamide. From the six compounds synthesized, four compounds I, II, III, and VI showed superior in antidiabetic activity compared to curcumin and other two compounds IV and V are inferior in antidiabetic activity compared to curcumin. Compound II was equal in activity compared to the standard drug glibenclamide. We developed nanoparticulate and liposomal delivery systems by encapsulating the curcumin. Curcumin nanoparticles were prepared by double emulsion (w/o/w) solvent evaporation method using poly-ε- caprolactone as the biodegradable polymer. Four different formulations (CNP1, CNP2, CNP3 and CNP4) were prepared by taking different drug to polymer ratios. Curcumin liposomes were prepared by thin film hydration – sonication method using soya lecithin and cholesterol as phospholipids. Four different formulations (CL1, CL2, CL3, and CL4) were prepared by taking different drug to lipid ratios. The prepared formulations were evaluated for particles size, surface potential, entrapment efficiency, Invitro release, drug polymer interaction.Particle size of all formulations was in the range of 300-470 nm and 110-240 nm; and the entrapment efficiencies were in the range of 75-85 % and 44-70 % for nanoparticles and liposomes respectively. From the formulations CNP3 and CL3 were selected as best formulations by considering the size, entrapment efficiency and release profiles. Pharmacokinetic parameters of the CNP3 and CL3 formulations were evaluated in rat. CNP3 and CL3 formulations were evaluated for hepatoprotective activity in CCl4 induced liver toxicity model and drug levels in different tissues including liver were determined. Formulation CNP3 showed better in vivo performance compared to CL3, curcumin IV and oral solutions. High liver levels of drug were achieved by the nanoparticular formulation (CNP3). Key words: Synthesis of curcumin, Screening of curcumin, Curcumin nanotechnology formulation
Authors and Affiliations
T. Srilatha*, K. Umasankar, P. Jayachandra Reddy, N. Srikar
Keywords
Related Articles
- EP ID EP118101
- DOI -
- Views 150
- Downloads 0
IN SILICO DESIGN AND MOLECULAR DOCKING STUDIES OF NOVEL PYRIDYL TRIAZOLE DERIVATIVES AS COX-2 INHIBITORS
ABSTRACT Molecular docking is used to predict and analyze interactions between protein receptors and ligands. In the present investigation novel substituted pyridyl triazoles are incorporated into benzothiazole a...
BIOANALYTICAL METHOD FOR THE QUANTITATIVE ESTIMATION OF FROVATRIPTAN IN RABBIT PLASMA BY LC–MS/MS AND ITS APPLICATION TO A PHARMACOKINETIC STUDY
ABSTRACT Liquid chromatography–tandem mass spectrometry was used to develop a simple, sensitive and rapid method for the quantitative determination of frovatriptan in rabbit plasma using frovatriptan d3 as intern...
PREPARATION AND CHARACTERIZATION OF DILTIAZEM BASE FROM ITS OFFICIAL SALT FORM
ABSTRACT Diltiazem hydrochloride (DTZ), a drug used in the treatment of angina pectoris is very popular for treatment of old age hypertension. The drug is well absorbed from GI tract, but its bioavailability is l...
ANTOBODY RESPONSE OF ACHYRANTHES ASPERA LINN. TO AEROMONAS HYDROPHILA IN OREOCHROMIS MOSSAMBICUS
ABSTRACT Fish is the cheapest and most easily digestible animal protein and was obtained from natural sources from time immemorial for consumption by human beings. Fish culture can be taken as a major economic ac...
SYNTHESIS , CHARACTERIZATION AND BIOLOGICAL ACTIVITY FOR BINUCLEAR COMPLEXES Co(II), Cu(II), Ni(II), Mn(II) and Hg(II) WITH SCHIFF BASE LIGAND TYPE N2O2
ABSTRACT The syntheses of some Ni(II),Co(II), Cu(II),Mn(II)and Hg(II) Schiff base complexes have been reported. The Schiff base ligand H2L (C28H20N2O2) under were prepared by the condensation of amine namely benz...