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Enhancement of anti‐inflammatory effects of biphenylylacetic acid by its incorporation into lipid microspheres

Using lipid microspheres (LM), average diameter 0.2 μm, and containing methyl and ethyl esters of biphenylylacetic acid (BPAA) in the carrageenan paw oedema tests in rats, it was found that their anti‐inflammatory activities were enhanced 3 to 8 times over that of free BPAA. By electron microscopy, LM were seen to be taken up into the endothelial cells of the blood vessels and macrophages at the inflamed sites. In a study using dogs, after an intravenous injection of BPAA‐methyl ester incorporated into LM (lipo‐BPAA‐Me), lipo‐BPAA‐Me rapidly disappeared from the blood and the BPAA serum level was gradually elevated. These results, together with previous findings, suggest that part of lipo‐BPAA‐Me was immediately transferred to the inflamed site and taken up by prostaglandin (PG)‐producing cells as macrophages. It is considered that the antiinflammatory effects of BPAA are enhanced by incorporating it into LM.