FORMULATION DEVELOPMENT AND CHARACTERIZATION OF TEA TREE OIL LOADED ETHOSOMES

To prepare ethosomes containing tea tree oil by hot homogenization method and to evaluate its physical characters and in-vitro release pattern.  the preformulation studies were carried out by standard procedure. The morphology of globule was studied by optical microscopy. The globule size and zeta potential was determined by Zetasizer, respectively and in-vitro study was done by diffusion method and the drug content was analyzed by HPTLC method. The release kinetics was also studied by fitting into few mathematical models.  All the formulations were showed spherical and unilamellar shape with globule size of 931 to 975 nm, the zeta potential in the range of – 40 to -52 mV and entrapment efficiency was 57 to 65 %. Finally the invitro release studies showed the drug release from the ethosomal vesicles was burst release at initial time followed by sustained release over throughout the study. From the above consideration of evaluation studies, the tea tree oil loaded ethosomal formulation F5 shows best globule size, zeta potential and entrapment efficiency. The sustained action was confirmed by invitro release studies. All the formulations are followed zero order drug release and diffusion type of mechanism of drug releases with Fickian model. Ethosome loaded tea tree oil could be the best choice for topical application

TARGETED DELIVERY OF SILYMARIN TO LIVER CELLS BY GALACTOSYLATED NANOPARTICLES: IN-VITRO & IN-VIVO EVALUATION STUDIES

Targeted delivery of drug to hepatic can be successfully achieved by binding to asialoglycoprotein receptor which is present in liver cells. For the targeting of liver cells, galactosylated chitosan nanoparticles were prepared and silymarin drug was loaded for the treatment of liver cirrhosis. The prepared galactosylated and chitosan nanoparticles were evaluated by physiochemical parameters like particles size, morphology, entrapment efficiency, zeta potential and invitro release studies. The successful formulation was subjected to invivo evaluation studies like organ drug distribution studies and Hepatoprotective activity by calculating SGOT, SGPT concentration. Based on plasma drug concentration profile, pharmacokinetics parameters like AUC, AUMC, Cmax, Tmax, t1/2, MRT & clearances were evaluated. The above results indicate galactosylated chitosan nanoparticles might be the best suitable carrier to target liver cells in treating liver cirrhosis

Transdermal Delivery of Insulin by Biodegradable Chitosan Nanoparticles: Exvivo and In vivo Studies: Transdermal delivery of insulin

Insulin-loaded biodegradable chitosan nanoparticle was prepared by the polyelectrolyte complex formation method. The prepared nanoparticles were in the size of 110 nm and had high entrapment (91.0%) capacity. The transdermal nanoinsulin was characterized by in vivo hypoglycemic effects. Plasma glucose was decreased to the range of 80.34 to 96.74 mg/dl, and insulin levels were increased to the range of 21.62to 45.80 μIU/ml for up to 60 h. The pharmacokinetic and pharmacodynamic parameters like AUC, Cmax, Tmax and relative bioavailability of transdermal patch loaded insulin-chitosan nanoparticles were 3153.36 μIU/ml/h, 45.80 μIU/ml, 8 h and 20.02%, respectively

Crystal structures of 1:1 complexes of meclofenamic acid with choline and ethanolamine

The hydrated 1:1 complex of meclofenamic acid with choline crystallites in the orthorhombic acid space group Pna2<SUB>1</SUB> with a = 9.637(1), b = 12.962(2), c = 33.099(4) Å and Z = 8 . Crystals of the corresponding anhydrous complex with ethanolamine are triclinic, space group P1̅, with a = 9.232(3), b = 12.287(5), c = 17.033(3) Å, α = 70.21(2), β = 76.72(2), γ = 68.21(3)° and Z = 4. The structures have been solved by direct methods and refined to R value of 0.062 and 0.079, respectively for 1942 and 2852 observed reflections. The four crystallographically independent meclofenamate anions in the complexes have nearly the same molecular geometry which in turn is very similar to that found in the crystal structure of free meclofenamic acid. The choline and ethanolamine molecules assume a gauche conformation with respect to the central C---C bond. The invariant structural features observed in the crystals of the free fenamates are retained by the meclofenamate ions in the complexes. These features are the rigid coplanar geometry of the six-membered ring carrying the carboxyl group, the carboxyl group and the imino nitrogen atom, and the internal hydrogen bond connecting the imino and the carboxyl groups. The crystal structures are stabilised by ionic interactions between the carboxylate groups of meclofenamate ions and choline or ethanolamine cations, and hydrogen bonds. The choline complex exhibits pseudosymmetry and the distribution of molecules in it is nearly centrosymmetric although the space group is noncentrosymmetric. The packing of molecules in the crystals is such that the polar columns are surrounded by non-polar regions. The core of each column in the choline complex is made up of water molecules connected by hydrogen bonds involving disordered protons. The results of the X-ray structure analysis of fenamates and their crystalline complexes provide some insights into structure-function relationships in this family of drugs

Crystal structures of 1:1 complexes of meclofenamic acid with choline and ethanolamine

The hydrated 1:1 complex of meclofenamic acid with choline crystallites in the orthorhombic acid space group P \bar{1} with a = 9.637(1), B = 12.962(5), C = 33.099(4) Å and Z = 8. Crystals of the corresponding anhydrous complex with ethanolamine are triclinic, space group Image , with a = 9.232(3), B = 12.287(5), C = 17.033(3) Å, \alpha = 70.21(2), \beta = 76.72(2), \gamma = 68.21(3)° and Z = 4. The structures have been solved by direct methods and refined to R value of 0.062 and 0.079, respectively for 1942 and 2852 observed reflections. The four crystallographically independent meclofenamate anions in the complexes have nearly the same molecular geometry which in turn is very similar to that found in the crystal structure of free meclofenamic acid. The choline and ethanolamine molecules assume a gauche conformation with respect to the central C---C bond. The invariant structural features observed in the crystals of the free fenamates are retained by the meclofenamate ions in the complexes. These features are the rigid coplanar geometry of the six-membered ring carrying the carboxyl group, the carboxyl group and the imino nitrogen atom, and the internal hydrogen bond connecting the imino and the carboxyl groups. The crystal structures are stabilised by ionic interactions between the carboxylate groups of meclofenamate ions and choline or ethanolamine cations, and hydrogen bonds. The choline complex exhibits pseudosymmetry and the distribution of molecules in it is nearly centrosymmetric although the space group is noncentrosymmetric. The packing of molecules in the crystals is such that the polar columns are surrounded by non-polar regions. The core of each column in the choline complex is made up of water molecules connected by hydrogen bonds involving disordered protons. The results of the X-ray structure analysis of fenamates and their crystalline complexes provide some insights into structure-function relationships in this family of drugs

Preparation and X-ray characterization of four new crystal forms of jacalin, a lectin from Artocarpus integrifolia

Four new crystal forms of the anti-T lectin from jackfruit (Artocarpus integrifolia) have been prepared and characterized. Three of them, two monoclinic (P21, A = 59·4 Å, B = 83·3 Å, C = 63·5 Å, β = 107·7°; C2, A = 106·1,Å, B = 53·9 Å, C = 128·0 Å, β = 95·0 Å) and one orthorhombic (C2221, A = 98·1 Å, B = 67·3 Å, C = 95·1 Å) were grown with 2-methylpentan-2,4-diol (MPD) as the precipitant while the fourth, an hexagonal from (P6122, A = b = 129·6 Å, C = 157·9 Å), was obtained in the presence of methyl-ga-D-galactopyranoside with polyethylene glycol 4000 as the precipitant. The reported relative molecular mass (Mr) of the lectin was found to be inconsistent with the solvent content of the crystals estimated using measured densities. The Mr was redetermined using size-exclusion chromatography in the presence of methyl-α-D-galactopyranoside and Ferguson-plot analysis of mobilities in polyacrylamide gel electrophoresis. The redetermined Mr (66,000) is consistent with the measured crystal densities. The orthorhombic and the hexagonal forms, which have one half molecule and one molecule, respectively, in the asymmetric unit, are suitable for high-resolution X-ray analysis

Preparation and x-ray characterization of four new crystal forms of Jacalin, a lectin from Artocarpus integrifolia

Four new crystal forms of the anti-T lectin from jackfruit (Artocarpus integrifolia) have been prepared and characterized. Three of them, two monoclinic (P21, A = 59·4 Å, B = 83·3 Å, C = 63·5 Å, β = 107·7°; C2, A = 106·1,Å, B = 53·9 Å, C = 128·0 Å, β = 95·0 Å) and one orthorhombic (C2221, A = 98·1 Å, B = 67·3 Å, C = 95·1 Å) were grown with 2-methylpentan-2,4-diol (MPD) as the precipitant while the fourth, an hexagonal from (P6122, A = b = 129·6 Å, C = 157·9 Å), was obtained in the presence of methyl-ga-Image -galactopyranoside with polyethylene glycol 4000 as the precipitant. The reported relative molecular mass (Mr) of the lectin was found to be inconsistent with the solvent content of the crystals estimated using measured densities. The Mr was redetermined using size-exclusion chromatography in the presence of methyl-α-Image -galactopyranoside and Ferguson-plot analysis of mobilities in polyacrylamide gel electrophoresis. The redetermined Mr (66,000) is consistent with the measured crystal densities. The orthorhombic and the hexagonal forms, which have one half molecule and one molecule, respectively, in the asymmetric unit, are suitable for high-resolution X-ray analysis