Tissue distribution and in vivo immunosuppressive activity of liposomal cyclosporine

K. Vadiei, G. Lopez-Berestein, R. Perez-Soler, D. R. Luke

Research output: Contribution to journalArticle

21 Scopus citations

Abstract

The distribution and immunosuppressive activity of liposomal cyclosporine (L-CSA) when administered iv as single- and multiple-doses were compared with the commercially available cyclosporine (C-CSA) in rats. CSA concentrations in the spleen and liver were significantly greater 1 hr after dosing in rats given L-CSA compared with C-CSA. The apparent tissue to blood partition coefficient at 1 hr after dosing was significantly greater for the liver and spleen of rats treated with L-CSA compared with C-CSA. Drug concentrations 24 hr after single doses of L-CSA were significantly lower in the kidney, heart, lung, and adipose tissues compared with animals given C-CSA. Lymphocyte-blastogenic response was studied in a separate group of rats given 10 mg/kg/day of L-CSA or C-CSA for 10 days compared with drug-free control groups. A 3-fold decrease in blastogenic response was observed in rats given L-CSA compared with C-CSA-treated rats (12.7 ± 11.8 vs. 34.9 ± 11.3 x 103 dpm/106 cells; p < 0.05). These data suggest that the liposomal formulation of CSA leads to enhanced tissue levels of CSA in the spleen coupled with augmentation in immunosuppressive activity.

Original languageEnglish (US)
Pages (from-to)1147-1151
Number of pages5
JournalDrug Metabolism and Disposition
Volume19
Issue number6
StatePublished - Jan 1 1991
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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