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PubMed2006

Characterization of pegylated copolymeric micelles and in vivo pharmacokinetics and biodistribution studies.

The aim of this study was to evaluate the influence of pegylated copolymeric micelle carrier on the biodistribution of drug in rats. The copolymers were synthesized via a modified ring-opening copolymerization of lactone monomers (epsilon-caprolactone, delta-valerolactone, L-lactide) and poly(ethylene glycol) (PEG(10,000) and PEG(4000)). The molecular weights and the polydispersities of synthesized copolymers were in the range of 15,000-31,000 g/mol and 1.7-2.7, respectively. All of the pegylated amphiphilic copolymers were micelles formed with low CMC values in the range of 10(-7)-10(-8)M. The drug-loaded micelles were prepared via a dialysis method. The average particle size of micelles was around 150-200 nm. The cytotoxicity in terms of cell viability after treated with PCL-PEG, PVL-PEG, and PLA-PEG micelles was insignificant. PCL-PEG and PVL-PEG micelles without branch side chain in structures had higher drug loading than PLA-PEG micelles. In vitro release profiles indicated the release of indomethacin from these micelles exhibited a sustained release behavior. The similar phenomenon was also observed in vivo in rats. The pegylated copolymeric micelles not only decreased drug uptake by the liver and kidney, but also prolonged drug retention in the blood.

Animals↗
PubMed1990

Competitive partial inhibitors of serum albumin-catalyzed sulfur cyanolysis.

Efforts to locate the active site for sulfur cyanolysis catalyzed by bovine serum albumin have led to systematic tests of several compounds that inhibit the catalyzed reaction. Hexanoate and 5-dimethylaminonaphthalene-1-sulfonate bind at the same site and are partial inhibitors competitive with cyanide, uncompetitive with respect to sulfur. Various dansyl amino acids and 1-anilino-8-naphthalene sulfonate display the same inhibitory behavior but bis (1-anilino-8-naphthalene sulfonate) is a total inhibitor competitive with cyanide. These findings are interpreted to indicate that the cyanolysis active site is near, but not at, one of the short-chain fatty acid binding sites on albumin subdomain 2-AB or 3-AB. Both ionic repulsion and steric considerations are implicated in the mechanisms of inhibition.

Anilino Naphthalenesulfonates↗
PubMed2006

Prostaglandin E2 receptor EP1 transactivates EGFR/MET receptor tyrosine kinases and enhances invasiveness in human hepatocellular carcinoma cells.

Recent evidence indicates that cyclooxygenase-2 (COX-2) and epidermal growth factor receptor (EGFR) are involved in hepatocarcinogenesis. This study was designed to evaluate the possible interaction between the COX-2 and EGFR signaling pathways in human hepatocellular carcinoma (HCC) cells. Immunohistochemical analysis using serial sections of human HCC tissues revealed positive correlation between COX-2 and EGFR in HCC cells (P < 0.01). Overexpression of COX-2 in cultured HCC cells (Hep3B) or treatment with PGE(2) or the selective EP(1) receptor agonist, ONO-DI-004, increased EGFR phosphorylation and tumor cell invasion. The PGE(2)-induced EGFR phosphorylation and cell invasiveness were blocked by the EP(1) receptor siRNA or antagonist ONO-8711 and by two EGFR tyrosine kinase inhibitors, AG1478 and PD153035. The EP(1)-induced EGFR transactivation and cell invasion involves c-Src, in light of the presence of native binding complex of EP(1)/Src/EGFR and the inhibition of PGE(2)-induced EGFR phosphorylation and cell invasion by the Src siRNA and the Src inhibitor, PP2. Further, overexpression of COX-2 or treatment with PGE(2) also induced phosphorylation of c-Met, another receptor tyrosine kinase critical for HCC cell invasion. Moreover, activation of EGFR by EGF increased COX-2 promoter activity and protein expression in Hep3B and Huh-7 cells, whereas blocking PGE(2) synthesis or EP(1) attenuated EGFR phosphorylation induced by EGF, suggesting that the COX-2/PGE(2)/EP(1) pathway also modulate the activation of EGFR by its cognate ligand. These findings disclose a cross-talk between the COX-2/PGE(2)/EP(1) and EGFR/c-Met signaling pathways that coordinately regulate human HCC cell invasion.

Alprostadil↗
PubMed1986

[Effect of 2-ethyl-2-ene-1-al and analogous compounds on the growth and ultrastructure of fungi].

Analogs of the natural substance (E)-hex-2-en-1-al which occurs naturally in green plants and is known to have microbiocidal properties were synthesized and studied with respect to their antifungal properties. Saturated and unsaturated aldehydes, alcohols, carbon acids and enolacetate were tested against various fungi by applying these compounds either over the gaseous phase or in suspension. The following ranking was observed on the basis of fungicidal activity: enolacetate of 2-ethylhex-2-enoic acid greater than 2-ethylhex-2-en-1-al greater than 2-ethylhex-2-en-1-al greater than 2-ethylhex-2-en-1-ol. Saturated analogs showed the same order of activity as the unsaturated ones, however, they were less efficient. The effects on the ultrastructural changes were analyzed in Mucor mucedo exposed to concentrations of the analogs that inhibited growth. Main effects were observed on mitochondrial and nuclear membranes. The kind of destruction caused by enolacetate of 2-ethylhex-2-en-1-al differed from the other substances tested. Aspects of the mode of action are discussed.

Acetates↗
PubMed2004

A biodegradable injectable thermoplastic for localized camptothecin delivery.

Camptothecin is an example of a potent drug with a short half-life that would benefit from a localized drug depot system that maintains its stability prior to being released. For this reason, a thermoplastic, biodegradable polymer drug depot was prepared and characterized, and the in vitro release of camptothecin examined. epsilon-Caprolactone oligomers were prepared by ring-opening polymerization initiated by various alcohols. The polymers were characterized via differential scanning calorimeter (DSC) for thermal transitions, and via a parallel plate rheometer for melt viscosity. Camptothecin was loaded into the oligomers and released into PBS buffer. The viscosity of the oligomers was alterable by the initiator used. The oligomers were semi-crystalline with melting points between 37 and 45 degrees C. Camptothecin was released from the oligomers in a diffusion-controlled manner, with the release rate increasing as the melt viscosity of the oligomer decreased. The unreleased camptothecin remained in its active lactone form for a period of up to 16 weeks.

Biocompatible Materials↗
PubMed1977

Aqueous chamber drug distribution volume measurement in rabbits.

A method was developed for aqueous chamber drug distribution volume measurement in the albino rabbit, and the apparent volume of distribution was determined for inulin, pilocarpine alkaloid, and 1-hexanoic acid. The method consists of injecting a suitable concentration of drug, in an appropriate volume of fluid, into the anterior chamber of the eye and monitoring the decline in drug concentration as a function of time by periodic sampling of the aqueous humor. Graphical analysis of the resulting data yields both the apparent volume of distribution and the turnover rate constant of the aqueous humor. The technique does traumatize the eye, causing formation of plasmoid aqueous, which does not interfere with the apparent drug distribution volume measurement or the determination of aqueous humor turnover. Inulin was used to determine the physiological aqueous volume, 287 mul, in good agreement with literature values. The turnover rate constant was 0.016 min-1, also in good agreement with literature values. The apparent volume of distribution for pilocarpine alkaloid was 575 mul in albino eyes and 760 mul in pigmented irides; for 1-hexanoic acid in albino eyes, it was 760 mul. For pilocarpine alkaloid, literature citations on the fraction of dose absorbed have been based on an assumed apparent volume of distribution of 250-300 mul. Therefore, a factor of two error has been introduced when using albino eyes and a factor of almost three has been introduced when using pigmented eyes. The implication of the apparent volume of distribution for pilocarpine in its ocular disposition is discussed, as is the unexpected observation that pilocarpine alkaloid apparently inhibits formation of plasmoid aqueous and follows one-compartment kinetics during these studies. Is is shown that the one-compartment kinetics for pilocarpine are due to its biological activity in the aqueous chamber.

Animals↗