PMID: 8954169Jan 1, 1996Paper

Lipophilic 1-beta-D-arabinofuranosyl cytosine derivatives in liposomal formulations for oral and parenteral antileukemic therapy in the murine L1210 leukemia model

Journal of Cancer Research and Clinical Oncology
Reto Schwendener, Herbert Schott

Abstract

The N4-alkylcytosine arabinoside derivative N4-octadecyl-AraC (AraC-Ocd, NOAC) and the (1-octadecylglycero-3-phospho)-AraC (Ocd-GroP-AraC, OPA) conjugate are new lipophilic derivatives of the cytostatic drug 1-beta-D-arabinofuranosylcytosine (AraC) that produce high antileukemic effects in the L1210 murine leukemia model when administered orally or parenterally as liposomal formulations. Between 83% and 100% of the treated animals were cured after five consecutive daily oral drug applications with a total dose of 1 mmol/kg AraC-Ocd or Ocd-GroP-AraC. Corresponding results were obtained after parenteral therapy on days 2 and 6 after tumor inoculation with five- to ten-fold lower concentrations of these two compounds. A comparable cytotoxic activity was found with the orally active AraC-5'-(n-stearyl phosphate). However, because of its strong hemolytic toxicity this derivative cannot be used for parenteral therapy. Another AraC conjugate, which was modified with two long-chain hydrocarbons, the (1-octadecylglycero-3-phospho)-N4-hexadecyl-AraC was, probably because of poor oral bioavailability, only active when applied parenterally. The new lipophilic AraC derivatives AraC-Ocd and Ocd-GroP-AraC are compounds with a high potential f...Continue Reading

References

May 28, 1992·International Journal of Cancer. Journal International Du Cancer·R A Schwendener, H Schott
Jan 15, 1986·International Journal of Cancer. Journal International Du Cancer·W RubasR Schwendener
Nov 1, 1971·Clinical Pharmacology and Therapeutics·D H Ho, E Frei

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Citations

May 21, 2005·Pharmaceutical Research·Laura M LandPaul Michael Bummer
Apr 15, 2004·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·R Neslihan Gursoy, Simon Benita
Jun 6, 2000·Advanced Drug Delivery Reviews·E MastrobattistaG Storm
Jun 7, 2000·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·T Gershanik, S Benita
Apr 29, 2000·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·E L VodovozovaJ G Molotkovsky
Jun 30, 2000·Clinical and Experimental Pharmacology & Physiology·T LockettR Whittaker
Aug 7, 2002·Clinical Pharmacokinetics·Akinobu HamadaMasahiro Nakano
Mar 1, 2012·Drug Development and Industrial Pharmacy·Md Akhlaquer RahmanZeenat Iqbal
Dec 22, 2007·Drug Development and Industrial Pharmacy·Deepa Patel, Krutika K Sawant
Nov 29, 2008·Journal of Colloid and Interface Science·Lijuan WangXuefeng Li
Jul 6, 2004·The Journal of Pharmacy and Pharmacology·V B PatravaleR M Kulkarni
Aug 23, 2005·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Alfred FahrMathew L S Leigh
Mar 19, 2013·International Journal of Pharmaceutics·Aled D Roberts, Haifei Zhang
Dec 3, 2014·International Journal of Pharmaceutics·Neus LozanoKostas Kostarelos
Nov 28, 2006·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Sheikh ShafiqMushir Ali
Aug 6, 2010·Pharmaceutical Development and Technology·Jaleh VarshosazFatemeh Akhavan Salamat
May 16, 2017·Artificial Cells, Nanomedicine, and Biotechnology·Usama AhmadSahabjada Siddiqui
Aug 17, 2021·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Maryam FallahHamed Mirzaei

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