EGCG derivatives aminopentyl dideoxyEGCG and aminopentyl dideoxygallocatechin-3-gallate (cis-APDOEGCG and trans-APDOEGCG) had an enhanced inhibitory effect on the proliferation when used at more than 30 mu M. To elucidate antiangiogenic effect of EGCG, we used a 1 mu M concentration for subsequent experiments where no selleck screening library effect on proliferation was observed. These EGCG derivatives showed a stronger
inhibitory effect on migration, invasion, and tube formation by HUVECs than the non-derivatized EGCG. Furthermore, the derivatives induced a change in the distribution of F-actin and subsequent morphology of the HUVECs. Next, we synthesized fluorescent TokyoGreen-conjugated EGCG derivative (EGCG-TG)
and observed the distribution in HUVECs under a confocal laser scanning microscope. Abundant fluorescence was observed in the cells after a 3-h incubation, and was localized in mitochondria as well FG-4592 as in cytoplasm. These results suggest that EGCG was incorporated into the HUVECs, that a portion of it entered into their mitochondria.”
“In this study, it was shown that the incorporation of superdisintegrants in solid dispersion tablets containing a high drug load can strongly enhance the dissolution rate of the highly lipophilic drug fenofibrate. In addition, the dissolution rate was more increased when the superdisintegrant was incorporated in the drug containing solid dispersions than when it was physically mixed with the solid dispersions. The dissolution rate enhancement strongly depended on the type of superdisintegrants and increased in the order Polyplasdone (R) XL-10 < Polyplasdone (R) XL << AS1842856 cell line Ac-Di-Sol (R) approximate
to Primojel (R). The dissolution behavior also depended on the type of hydrophilic carriers. Solid dispersion tablets based on inulin 4 kDa, polyethylene glycol 20 K and polyvinylpyrrolidone K30 showed a much faster dissolution than those based on mannitol and hydroxypropyl-beta-cyclodextrin. Finally, inulin 4 kDa-based solid dispersion tablets showed excellent storage stability, while polyethylene glycol 20 K-and polyvinyl pyrrolidone K30-based solid dispersion tablets did not. (c) 2009 Elsevier B.V. All rights reserved.”
“The influence of intragranular excipients (lactose or dicalcium phosphate) and the drying procedure and conditions (oven-drying and freeze-drying after freezing at -30 or -196 degrees C) on the properties of tablets of MCC-Carbopol (R) pellets was evaluated. The drying procedure caused remarkable differences in pellet size and porosity (freeze-dried pellets were 3-fold more porous than those oven dried). Theophylline release from pellets was completed in less than 30 min and followed first-order kinetics, with a rate closely related to the intragranular porosity.