[Organ specific application of drugs by means of cellular capsule systems (author's transl)].
It is suggested to use living cells (red blood cells, lymphocytes and leucocytes) as drug delivery systems for temporal and spatial drug administration in human therapeutics and diagnosis. The effectiveness of drug loaded cells is demonstrated for the drug methotrexate which is used in cancer treatment. Red blood cells are loaded with methotrexate using the dielectric breakdown technique. Dielectric breakdown leads to a transient increase of permeability of the cell membrane. Red blood cells loaded with tritium-labelled methotrexate were injected into mice and the activity level was measured in several organs as a function of time. It is shown that with this drug delivery system more than 50% of the drug (after 10 min) can be accumulated in the liver and that a high activity level can be sustained in this or gan for more than 3 hours. On the other hand, administration of this drug by injecting solutions in the usual manner leads only to an 25% accumulation of methotrexate (after 10 min) in the liver. The drug is excreted completely after 1 to 2 hours. It is proposed to load red blood cells simultaneously with para- or ferromagnetic substances to obtain organ-specificity for any selected site of the body.
D000818:Animals; D002463:Cell Membrane Permeability; D004912:Erythrocytes / Q000378:metabolism*; D007700:Kinetics; D008099:Liver / Q000378:metabolism; D008727:Methotrexate / Q000008:administration & dosage* / Q000097:blood / Q000378:metabolism; D051379:Mice; D009928:Organ Specificity; D013997:Time Factors
D008727:Methotrexate
Organspezifische Applikation von pharmazeutisch aktiven Substanzen über zellulare Trägersysteme