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  • 1
    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
    Library Location Call Number Volume/Issue/Year Availability
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  • 2
    ISSN: 1432-0843
    Keywords: 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
    Library Location Call Number Volume/Issue/Year Availability
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Cancer chemotherapy and pharmacology 32 (1993), S. 90-95 
    ISSN: 1432-0843
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Conclusion From the foregoing it is evident that the experimental profile of miltefosine and alkylphosphocholines is different from that of conventional anticancer agents. Much evidence indicated that the mode of action of alkylphosphocholines was related to plasma-membrane-associated phosphoinositide metabolism. Inhibition of phospholipase C and/or PKC is currently thought to be the main biochemical target of alkylphosphocholines. Considering the great importance of both phosphoinositide metabolism and the regulation of a broad spectrum of cellular functions, including differentiation and invasion, miltefosine could become an interesting new drug. In addition, it may be a tool for further studies into the biochemical pathway of signal transduction in malignant cells.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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