Oussoren C, Storm G
Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, The Netherlands.
Pharm Res. 1997 Oct;14(10):1479-84. doi: 10.1023/a:1012145410859.
The aim of the present paper was to assess the effect of inclusion of distearoylphosphatidylethanolamine-poly(ethyleneglycol) (DSPE-PEG) into liposomal bilayers on the lymphatic uptake and lymph node localization of liposomes after subcutaneous administration.
[3H]-Cholesteryloleylether labeled liposomes of various composition and sizes were injected s.c. into the dorsal side of the foot of rats. At several time-points after injection, blood levels of liposomes were determined. Lymphatic uptake from the s.c. site of injection and lymph node localization in regional lymph nodes were determined at the end of the 52 h observation period.
The results demonstrate that inclusion of DSPE-PEG into several types of liposomes has only a modest effect on lymphatic uptake. Also lymph node localization is only slightly affected by PEG-mediated steric stabilization.
Factors other than the presence of a steric barrier are more important in determining lymphatic uptake from the s.c. injection site. The observation that lymph node localization was only slightly affected by PEG-coating strongly suggests that macrophage uptake is not the only important mechanism of lymph node localization of s.c. administered liposomes.
本文旨在评估将二硬脂酰磷脂酰乙醇胺-聚乙二醇（DSPE-PEG）纳入脂质体双层对皮下给药后脂质体的淋巴摄取及淋巴结定位的影响。
将不同组成和大小的[3H] -胆固醇油醚标记脂质体皮下注射到大鼠足背。注射后在多个时间点测定脂质体的血药浓度。在52小时观察期结束时，测定注射部位皮下的淋巴摄取及区域淋巴结中的淋巴结定位情况。
结果表明，在几种类型的脂质体中加入DSPE-PEG对淋巴摄取仅有适度影响。同样，淋巴结定位也仅受到PEG介导的空间稳定化的轻微影响。
在决定皮下注射部位的淋巴摄取方面，除了存在空间屏障外，其他因素更为重要。PEG包被仅轻微影响淋巴结定位这一观察结果强烈表明，巨噬细胞摄取并非皮下给药脂质体淋巴结定位的唯一重要机制。
