K. Carlsson et al., LOCALIZATION OF TROXERUTIN IN THE VENOUS WALL MEASURED USING LASER-SCANNING MICROSCOPE, Journal des maladies vasculaires, 21, 1996, pp. 270-274
The vein wall is nourished by diffusion of blood nutrients from the lu
men and from the vasa vasorum. It is likely that drugs take the same w
ays to reach and diffuse through the vessel wall. Thus the uptake of a
drug with affinity for the vein wall should give information on its t
ransport to the tissue. This study aimed to explore troxerutin uptake
by the long saphenous vein. Troxerutin is a naturally fluorescent flav
onoid which has been known to improve subjective signs of patients wit
h chronic venous insufficiency. Nine patients undergoing surgical trea
tment of varicosis were enrolled in the study. They received for the l
ast 4 days before surgery either 3 500 mg of troxerutin (n = 4) or 1 0
00 mg twice daily (n = 2). Three patients as controls did not receive
any drug. Two samples from tigh and claf long saphenous vein were harv
ested in each patients and investigated with a confocal laser scanning
microscope developped by our institute measuring the fluorescence emi
tted by troxerutin after excitation by a 458 nm wavelength laser-beam.
The intensity of the overall fluorescence was significantly higher in
the treated groups (p < 0.001) and slightly higher in the patient who
received 3 500 mg of troxerutin than with the lower dosage. The outer
wall region provided the highest fluorescence in the treated group wh
ile a significant difference was observed in the fluorescence of the m
edial region between treated and control group. These results showed a
marked affinity of troxerutin for the venous wall. The highest uptake
in the outer wall region is likely to result from transport through v
asa vasorum, owing to the rheologic properties of the drug. The signif
icant medial fluorescence may account for the venous tone improvement
with the drug.