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  • 1
    Electronic Resource
    Electronic Resource
    Preparation and properties of the immunoconjugate composed of anti-human colon cancer monoclonal antibody and mitomycin C-dextran conjugate (1992)
    s.l. : American Chemical Society
    Bioconjugate chemistry 3 (1992), S. 132-137 
    Details
    ISSN: 1520-4812
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/bc00014a007
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  • 2
    Electronic Resource
    Electronic Resource
    Analysis of Drug Permeation Across Caco-2 Monolayer: Implication for Predicting In Vivo Drug Absorption (1997)
    Springer
    Pharmaceutical research 14 (1997), S. 486-491 
    Details
    ISSN: 1573-904X
    Keywords: Caco-2 monolayer ; intestinal membrane ; drug lipophilicity ; in vitro drug permeability ; in vivo drug absorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The aim of the present work is to characterize in vitro drug permeation processes across Caco-2 monolayer and to identify the advantages of this cultured cell system in predicting in vivo drug absorption after oral administration. Methods. The passive permeability of various drugs through Caco-2 monolayer was measured using Ussing-type chambers and compared with that of the isolated rat jejunum and colon. The in vivo drug permeability to the intestinal membrane was estimated by means of an intestinal perfusion study using the rat jejunum. Results. In Caco-2 monolayer, drug permeability increased with increasing drug lipophilicity and showed a good linear relationship with the in vivo permeability. In contrast, in the isolated jejunum and colon, the permeability of high lipophilic drugs was almost constant and, propranolol, a drug with the highest lipophilicity, hardly passed through the jejunal membrane in vitro. As a result, there was no significant relationship between in vitro and in vivo drug permeability in rat jejunum. However, the amount of drugs accumulated in the jejunal mucosa increased with increasing drug lipophilicity even under the in vitro condition. Conclusions. The permeation and the accumulation studies suggested that the rate-limiting process of in vitro permeation of lipophilic drugs through the intestinal membrane differs from that of in vivo drug absorption. On the other hand, drug permeation through Caco-2 monolayer, which consists of an epithelial cell layer and a supporting filter, is essentially the same process as that of in vivo drug absorption. We concluded that the simple monolayer structure of a cultured cell system provides a distinct advantage in predicting in vivo drug absorption.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1012103700981
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  • 3
    Electronic Resource
    Electronic Resource
    Enhanced Membrane Permeability to Phenol Red by Medium-Chain Glycerides: Studies on the Membrane Permeability and Microviscosity (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 309-312 
    Details
    ISSN: 1573-904X
    Keywords: enhancement of membrane permeability ; uptake into liposomes ; membranous microviscosity ; medium-chain glyceride ; cholesterol ; phenol red
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract To clarify the mechanism of the drug absorption enhancement by medium-chain glycerides (MCG), the changes in membrane permeability provoked by MCG were investigated with liposomal uptake experiments. Uptake of phenol red (PR) into liposomes increased with an increase in MCG content in the liposomal membrane, suggesting that PR absorption was enhanced in the “transcellular route.” However, the apparent membranous microviscosity obtained in fluorescence depolarization studies tended to increase with the addition of MCG in both the hydrophobic core and the polar head regions of the liposomal membrane. Thus, an enhancement in membrane permeability caused by MCG was not accompanied by a decrease in the apparent membranous microviscosity.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015982805718
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  • 4
    Electronic Resource
    Electronic Resource
    Disposition Characteristics of Macromolecules in Tumor-Bearing Mice (1990)
    Springer
    Pharmaceutical research 7 (1990), S. 339-346 
    Details
    ISSN: 1573-904X
    Keywords: Macromolecular compounds ; physicochemical characteristics ; tumor targeting ; systemic disposition ; hepatic uptake ; urinary excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract As part of the strategy for the design of macromolecular carriers for drug targeting, the disposition characteristics of macromolecules were studied in mice bearing tumors that served as target tissues. Eight kinds of macromolecules including four polysaccharides and four proteins with different molecular weights and electric charges were used; tissue distribution and tumor localization after intravenous injection were studied. Pharmacokinetic analysis revealed that the tissue radioactivity uptake rate index calculated in terms of clearance was different among the tested compounds; especially, the urinary radioactivity excretion clearances and the total hepatic radioactivity uptake clearances varied widely. Compounds with low molecular weights (approximately 10 kD) or positive charges showed lower tumor radioactivity accumulation; radioactivity was rapidly eliminated from the plasma via rapid urinary excretion or extensive hepatic uptake, respectively. On the other hand, large and negatively charged compounds, carboxymethyl dextran, bovine serum albumin, and mouse immunoglobulin G, showed higher radioactivity accumulation in the tumor (calculated total amounts were 15.6, 10.8, and 20.8% of the dose, respectively) and prolonged retention in the circulation. These results demonstrated that the total systemic exposure rather than the uptake rate index was correlated with total tumor uptake. Molecular weight and electric charge of the macromolecules significantly affected their disposition characteristics and, consequently, determined radioactivity accumulation in the tumor. It was concluded that a drug–carrier complex designed for systemic tumor targeting should be polyanionic in nature and larger than 70,000 in molecular weight.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015807119753
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  • 5
    Electronic Resource
    Electronic Resource
    Hepatic Disposition Characteristics of Electrically Charged Macromolecules in Rat in Vivo and in the Perfused Liver (1991)
    Springer
    Pharmaceutical research 8 (1991), S. 437-444 
    Details
    ISSN: 1573-904X
    Keywords: electric charge ; model macromolecule ; hepatic disposition ; cellular localization ; constant infusion ; adsorptive endocytosis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The effect of electric charge on the hepatic disposition of macromolecules was studied in the rat. Charged derivatives of dextran (T-70) and bovine serum albumin (BSA), mitomycin C–dextran conjugates (MMC-D), and lactosaminated BSA (Lac-BSA) were employed as model macromolecules. After intravenous injection, cationic macromolecules were rapidly eliminated from plasma because of their extensive hepatic uptake, while anionic and neutral macromolecules were slowly eliminated. Cationic macromolecules were recovered from parenchymal and nonparenchymal hepatic cells at a cellular uptake (per unit cell number) ratio of 1.4–3.2, while that of Lac-BSA was 14. During liver perfusion using a single-pass constant infusion mode, cationic macromolecules were continuously extracted by the liver, with extraction ratios at steady-state (E ss) ranging between 0.03 and 0.54, whereas anionic and neutral macromolecules were almost completely recovered in the outflow at steady state. The E ss for cationized BSA (Cat-BSA) and cationic MMC-Dcat were concentration dependent and decreased at low temperatures and in the presence of colchicine and cytochalasin B. The possible participation of the internalization process in the uptake of cationic macromolecules by hepatocytes was suggested.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015886708598
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  • 6
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of the hepatobiliary transport of bromphenol blue as a model of organic anionic compounds (1974)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 2 (1974), S. 495-509 
    Details
    ISSN: 1573-8744
    Keywords: hepatobiliary transport ; rat ; bromphenol blue ; pharmacokinetics ; roles of liver cytoplasmic Y- and Z-binding proteins and T binder
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A new pharmacokinetic model is proposed to explain the hepatobiliary transport of a nonmetabolized sulfonic acid dye, bromphenol blue, which is actively transported from the bloodstream into bile. This model has the advantage of taking into account the roles of the liver cytoplasmic Y- and Z- binding proteins and T binder.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01070944
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  • 7
    Electronic Resource
    Electronic Resource
    An application of water-in-oil and gelatin-microsphere-in-oil emulsions to specific delivery of anticancer agent into stomach lymphatics (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 241-255 
    Details
    ISSN: 1573-8744
    Keywords: drug delivery system for cancer chemotherapy ; anticancer agent ; water-in-oil emulsion ; microsphere-in-oil emulsion ; stomach wall ; improvement of availability in the lymphatics ; prolonged release ; reduction of adverse effect ; adjuvant chemotherapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The efficiency of water-in-oil (W/O) and gelatin-microsphere-in-oil (W/O-G) emulsions as drug delivery systems for achieving specificity into lymphatics was evaluated in the rat stomach. Following injection into the stomach wall, radioactivities of 131 I-labeled o-iodohippuric acid (IH, watersoluble model compound) and [ 14 C]tripalmitin (TP, tracer of oil) in blood, regional lymph nodes, thoracic lymph, and stomach were determined. Since increased transfer of TP indicated the facilitation of lymphatic transport of IH following injection of W/O and W/O-G emulsions, the existence of a special transport mechanism through which drug and oil are delivered together was confirmed for this injection site. W/O and W/O-G emulsions increased the concentration-time curve (AUC) of IH in the regional lymph nodes (1.7 and 5.5 times that of aqueous solution injection, respectively), so the improvement of bioavailability was accomplished. In addition, a prolonged release of IH and decrease of its maximum blood concentration were obtained following injection of W/O-G emulsion. These results suggest that W/O and W/O-G emulsions satisfy many of the criteria of an ideal drug delivery system for cancer chemotherapy. An abundant supply of lymphatic vessels in the stomach wall exhibited the efficiency of these delivery systems more clearly than did thigh muscle.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01065398
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  • 8
    Electronic Resource
    Electronic Resource
    Disposition and Tumor Localization of Mitomycin C–Dextran Conjugates in Mice (1987)
    Springer
    Pharmaceutical research 4 (1987), S. 293-300 
    Details
    ISSN: 1573-904X
    Keywords: mitomycin C–dextran conjugate ; polymeric prodrug ; tissue distribution ; tumor localization ; physicochemical characteristics ; antitumor activity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Mitomycin C–Dextran conjugates (MMC-D) were intravenously (iv) injected in mice bearing subcutaneous sarcoma 180. The tissue distribution was determined for three 14C-labeled anionic conjugates (MMC-Dan) with molecular weights of 10, 70, and 500 kd and one cationic 70-kd 14C-conjugate (MMC-Dcat). The anionic conjugates were slowly cleared from the plasma, and their elimination rate decreased with increasing molecular weight. Radioactivity accumulated in liver, spleen, lymph nodes, and tumor but not in heart, lung, intestines, kidney, or muscle after iv injection of all types of 14C-MMC-Dan. In contrast, the cationic conjugate was rapidly cleared from the plasma and accumulated mostly in the liver and spleen, while tumor levels remained low. The antitumor effect of the 70-kd MMC-Dan, which afforded the highest tumor concentration, was superior to that of free MMC. Therefore, anionic mitomycin C–dextran conjugates with a high molecular weight may be useful for tumor targeting in cancer chemotherapy.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016489002393
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  • 9
    Electronic Resource
    Electronic Resource
    Assessment of Drug Disposition in the Perfused Rat Brain by Statistical Moment Analysis (1991)
    Springer
    Pharmaceutical research 8 (1991), S. 683-689 
    Details
    ISSN: 1573-904X
    Keywords: blood–brain barrier ; moment analysis ; brain perfusion ; indicator dilution
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Drug disposition in the brain was investigated by statistical moment analysis using an improved in situ brain perfusion technique. The right cerebral hemisphere of the rat was perfused in situ. The drug and inulin were injected into the right internal carotid artery as a rapid bolus and the venous outflow curve at the posterior facial vein was obtained. The infusion rate was adjusted to minimize the flow of perfusion fluid into the left hemisphere. The obtained disposition parameters were characteristics and considered to reflect the physicochemical properties of each drug. Antipyrine showed a small degree of initial uptake. Therefore, its apparent distribution volume (V i) and apparent intrinsic clearance (CLint,i) were small. Diazepam showed large degrees of both influx and efflux and, thus, a large Vi. Water showed parameters intermediate between those of antipyrine and those of diazepam. Imipramine, desipramine, and propranolol showed a large CLint,i compared with those of the other drugs. The extraction ratio of propranolol significantly decreased with increasing concentrations of unlabeled propranolol in the perfusion fluid. These findings may be explained partly by the tissue binding of these drugs. In conclusion, the present method is useful for studying drug disposition in the brain.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015833513567
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  • 10
    Electronic Resource
    Electronic Resource
    Synthesis and Pharmacokinetics of a New Liver-Specific Carrier, Glycosylated Carboxymethyl-Dextran, and Its Application to Drug Targeting (1993)
    Springer
    Pharmaceutical research 10 (1993), S. 1253-1261 
    Details
    ISSN: 1573-904X
    Keywords: drug targeting ; sugar recognition ; glycosylated dextran ; pharmacokinetics ; cytosine β-D-arabinoside
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract To develop a new carrier system for hepatic targeting, carboxymethyl-dextran (CMD) was modified with galactose and mannose residues (Gal-CMD, Man-CMD), and their disposition characteristics were studied in mice using 14C-labeled dextran. At a dose of 1 mg/kg, i.v.-injected Gal-CMD and Man-CMD rapidly accumulated in the liver parenchymal and nonparenchymal cells, respectively, because of their preferential uptake via carbohydrate receptors in these cells. Pharmacokinetic analysis revealed that their uptake rates were sufficiently large for selective drug targeting. Targeting of cytosine β-D-arabinoside (araC) was studied using Gal-CMD as a specific carrier to the hepatocytes. From the conjugate of araC with Gal-CMD, araC was released with a half-life of 36 hr in phosphate buffer (pH 7.4) and 23 hr in plasma. An in vivo biodistribution study demonstrated a disposition profile of the conjugated araC similar to that of the carrier, and selective delivery to hepatocytes of up to 80% of the dose was achieved. These findings suggest that glycosylated CMDs are carriers with a high affinity to liver parenchymal or nonparenchymal cells without any affinity to other tissues.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1018949109004
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