Pharmacokinetic behavior and antineoplastic activity of liposomal hexadecylphosphocholine

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. i...

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Bibliographic Details
Published in:Cancer chemotherapy and pharmacology 1994, Vol.34 (5), p.393-398
Main Authors: KAUFMANN-KOLLE, P, DREVS, J, BERGER, M. R, KÖTTING, J, MARSCHNER, N, UNGER, C, EIBL, H
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Antineoplastic agents
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - pharmacokinetics
Antineoplastic Agents - therapeutic use
Biological and medical sciences
Body Weight - drug effects
Chemotherapy
Chromatography, High Pressure Liquid
Drug Carriers
Female
Half-Life
Injections, Intravenous
Liposomes
Mammary Neoplasms, Experimental - chemically induced
Mammary Neoplasms, Experimental - drug therapy
Medical sciences
Methylnitrosourea
Pharmacology. Drug treatments
Phosphorylcholine - administration & dosage
Phosphorylcholine - analogs & derivatives
Phosphorylcholine - pharmacokinetics
Phosphorylcholine - therapeutic use
Rats
Rats, Sprague-Dawley
Rats, Wistar
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Summary: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-gly-cero-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.).
ISSN:0344-5704
1432-0843
DOI:10.1007/BF00685563