Cellular uptake of a fluid-phase marker by human neutrophils from solutions and liposomes.
In assessing the feasibility of utilizing the phagocytic activity of polymorphonuclear leukocytes (PMNs) for a more efficient drug delivery to the cell, the uptake of the fluid-phase marker lucifer yellow CH (LY) at 37 degrees C by human PMNs from LY-containing liposomes was compared with that from solutions. In the presence of 10% autologous serum, the LY uptake at 37 degrees C via phagocytosis of a given PMN source when the concentrations of PMN, LY, and total lipid were in the range of 10(7) cells/ml, 0.5 mg/ml, and 50 mumol/ml, respectively. As expected, the LY uptake via phagocytosis was critically dependent upon the LY entrapment efficiency in the liposome preparation. Interestingly, little LY uptake was found when the serum was heat inactivated (56 degrees C x 30 min). The serum effect was upon liposome vesicles rather than upon the cells. The present study demonstrates that the use of particular drug carriers for targeted drug delivery to PMNs and possible to an extravascular site mediated by the cell infiltration is a viable approach.
Scieszka
J F
JF
Drug Delivery Systems Research, Upjohn Company, Kalamazoo, Michigan 49001.
Cho
M J
MJ
D000328:Adult; D005456:Fluorescent Dyes; D006801:Humans; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000378:metabolism; D008081:Liposomes; D008297:Male; D008875:Middle Aged; D009504:Neutrophils / Q000378:metabolism*; D010587:Phagocytosis / Q000187:drug effects; D010873:Pinocytosis / Q000187:drug effects; D012996:Solutions; D013050:Spectrometry, Fluorescence
D005456:Fluorescent Dyes; D007546:Isoquinolines; D008081:Liposomes; D012996:Solutions; C017475:lucifer yellow