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  • 1
    ISSN: 1573-7217
    Keywords: hexadecylphosphocholine ; human breast carcinoma ; pharmacokinetics ; sterically stabilized liposomes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The pharmacokinetics of free and different liposomal formulations of hexadecylphosphocholine (HPC) was investigated in tumor-bearing (human mammary tumor MaTu) and tumor-free mice after intravenous and intraperitoneal administration. The levels of HPC were evaluated at different times in serum, normal tissues, and tumor. The purpose was to test the hypothesis that the enhanced therapeutic efficacy of sterically stabilized HPC liposomes in comparison to conventional vesicles and free HPC is due to its pharmacokinetics. Conventional non-compartmental pharmacokinetic analysis and an elaborate three- and four-compartmental model were used for explaining the experimental data. The serum levels of HPC obtained with sterically stabilized liposomes were only consistently higher in comparison to conventional vesicles and free HPC in the first 4 h. In the xenografted MaTu carcinoma, the differences of the HPC content between the different groups are unexpectedly low and do not reflect the high therapeutic activity [5] of sterically stabilized HPC liposomes. Detailed analysis shows that the liposomally encapsulated drug displays a modified pharmacokinetic behavior, which may also involve lymphatic absorption of the liposomal drug.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Breast cancer research and treatment 43 (1997), S. 237-246 
    ISSN: 1573-7217
    Keywords: alkylphosphocholine ; hexadecylphosphocholine ; human breast carcinoma ; sterically stabilized liposomes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract New sterically stabilized liposomes derived from the antitumoragent hexadecylphosphocholine with reduced uptake by the mononuclearphagocyte system and improved antitumor activities were developedand tested. The bilayer of such sterically stabilizedliposomes consists of hexadecylphosphocholine, cholesterol and polyethylene glycol-linkedphosphoethanolamine. The measurement of carbon clearance in miceshows that these stabilized liposomes, in contrast toconventional alkylphosphocholine liposomes, are not largely engulfed bythe mononuclear phagocyte system. Their therapeutic activity onexperimental human breast carcinomas MaTu, MT-1 and MT-3was tested in nude mice. Especially in theMaTu models the sterically stabilized hexadecylphosphocholine liposomes resultedin significantly reduced tumor growth in comparison toconventional hexadecylphosphocholine liposomes or free hexadecylphosphocholine. The enhancedtherapeutic efficacy of sterically stabilized hexadecylphosphocholine liposomes isprobably related to the extended circulation time ofthe formulation and its accumulation in tumors.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1573-7217
    Keywords: alkykphosphocholines ; breast carcinoma ; eicosanylphosphocholine ; hexadecylphosphocholine ; liposomes ; nude mice ; octadecylphosphocholine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary This study examines thein vitro andin vivo activity of alkylphosphocholines (APC) in experimental human breast carcinomas. Three analogs, hexadecylphosphocholine (HPC), octadecylphosphocholine (OPC) and eicosanylphosphocholine (EPC) were investigated. Three hormone receptor negative cell lines were sensitive to all three APCsin vitro whereas the receptor positive MCF-7 line was more resistant. Sensitivity was seen in 4/6 hormone receptor negative tumorsin vivo, with HPC being the most active analog. There were no antitumor effects in the four receptor positive models. The reasons for these differences in response between hormone receptor negative and -positive lines are not yet understood and require further study. Gastrointestinal toxicity and hemolysis, the major side effects of the APCs, were reduced by the use of liposomal preparations.
    Type of Medium: Electronic Resource
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