通过将联苯乙酸包封于脂质微球中来增强其抗炎作用。

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

作者信息

Shoji Y, Mizushima Y, Yanagawa A, Shiba T, Takei H, Fujii M, Amino M

出版信息

J Pharm Pharmacol. 1986 Feb;38(2):118-21. doi: 10.1111/j.2042-7158.1986.tb04523.x.

DOI:10.1111/j.2042-7158.1986.tb04523.x

Abstract

Using lipid microspheres (LM), average diameter 0.2 micron, 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 anti-inflammatory effects of BPAA are enhanced by incorporating it into LM.

摘要

在大鼠角叉菜胶足爪水肿试验中，使用平均直径为0.2微米的脂质微球（LM），其在角叉菜胶中含有联苯乙酸（BPAA）的甲酯和乙酯，发现它们的抗炎活性比游离BPAA增强了3至8倍。通过电子显微镜观察，发现LM被炎症部位的血管内皮细胞和巨噬细胞摄取。在一项使用犬的研究中，静脉注射掺入LM的BPAA甲酯（lipo - BPAA - Me）后，lipo - BPAA - Me迅速从血液中消失，BPAA血清水平逐渐升高。这些结果与先前的发现一起表明，部分lipo - BPAA - Me立即转移到炎症部位，并被作为巨噬细胞的前列腺素（PG）产生细胞摄取。据认为，将BPAA掺入LM可增强其抗炎作用。