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  • Blood-brain barrier  (1)
  • Key words: Liposomes – Alkylphosphocholine – Pharmacokinetics  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Pharmacokinetic behavior and antineoplastic activity of liposomal hexadecylphosphocholine (1994)
    Springer
    Cancer chemotherapy and pharmacology 34 (1994), S. 393-398 
    Details
    ISSN: 1432-0843
    Keywords: Key words: Liposomes – Alkylphosphocholine – Pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract. Hexadecylphosphocholine (HePC) shows remarkable antineoplastic efficacy in Sprague-Dawley rats bearing methylnitrosourea-induced mammary carcinoma. Unfortunately, this is accompanied by detrimental side effects that include gastrointestinal damage, body weight loss, and thrombophlebitis after i. v. injection, which has precluded the use of the HePC in humans, where nausea and vomiting can occur at noneffective dose levels. We have developed small unilamellar vesicles (SUVs) composed of HePC, cholesterol, and 1,2-dipalmitoyl-sn-glycero-3-phosphoglycerol, which can be given p. o. and i. v. In contrast to the free drug, the toxicity of liposomal HePC is shown to be greatly reduced, and there is no risk of thrombophlebitis. Single administration of equimolar HePC doses results in differing pharmacokinetic values for free HePC (p. o.) and HePC-SUVs (p. o., i. v.).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00685563
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Blut-Hirnschranke und Penetration von Zytostatika (1985)
    Springer
    Journal of molecular medicine 63 (1985), S. 565-571 
    Details
    ISSN: 1432-1440
    Keywords: Blood-brain barrier ; Drug transfer ; Alkylglycerols
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The penetration of 12 commonly used anticancer agents through the blood-brain barrier (BBB) was measured in a rat model using a single-injection tissue-sampling technique. Two of the tested drugs penetrated the barrier, but only to a limited extent. Entry of the drugs into the brain tissue critically depends on molecular weight and lipophilia of the respective test compound. For drugs with a molecular weight of less than 500, BBB simply behaves like an oil/water interphase, whereas drugs with a molecular weight greater than 500 are practically excluded from transport through the BBB even if they show a favourable oil/water partition coefficient. However, permeability of cytostatics was strongly increased if short chain alkylglycerols, up to final concentrations of about 0.3 mol/l were added to the injected solution. Under these conditions the Brain-Uptake-Index (BUI) reached values up to about 50% (cyclophosphamide), depending on lipid solubility and molecular dimension of the respective test compound and the alkyl chain length of the glycerol derivative.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01733202
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
    Fulltext
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