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Simple screening methods for prediction of intestinal lymphatic transport of lipophilic drugs

Aims To compare the degree of uptake of lipophilic compounds by chylomicrons ex-vivo and by chylomicron-like artificial emulsion in-vitro to the corresponding intestinal lymphatic bioavailability reported in rats. To evaluate the utilization of these correlations as a predictive measurement of the lymphatic bioavailability potential of lipophilic drugs. Methods 9 lipophilic compounds (listed in Table 1) at a concentration of 1.75 × 10-6 M were incubated for 1 hour with chylomicrons separated from rat blood or with commercially available artificial chylomicron-like emulsion at pH 7.4. The lymphatic bioavailability of tested compounds reported in-vivo in rats was correlated with the degree of uptake by chylomicrons ex-vivo and by chylomicronlike emulsion in-vitro.