Munekane Masayuki, Mori Hinako, Takada Nao, Sano Kohei, Yamasaki Toshihide, Tanaka Toru, Sasaki Naoto, Rikitake Yoshiyuki, Mukai Takahiro
Laboratory of Biophysical Chemistry, Kobe Pharmaceutical University, 4-19-1 Motoyamakita-machi, Higashinada-ku, Kobe 658-8558, Japan; Graduate School of Medical Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.
Laboratory of Biophysical Chemistry, Kobe Pharmaceutical University, 4-19-1 Motoyamakita-machi, Higashinada-ku, Kobe 658-8558, Japan.
Nucl Med Biol. 2023 Nov-Dec;126-127:108388. doi: 10.1016/j.nucmedbio.2023.108388. Epub 2023 Sep 26.
Macrophage infiltration is a characteristic feature of atherosclerotic plaque progression. Since liposomes containing 1,2-distearoyl-sn-glycero-3-phosphoglycerol (DSPG) are efficiently phagocytosed by macrophages, we deduced that radiolabeled liposomes containing DSPG could potentially be used for nuclear imaging of vulnerable atherosclerotic plaques. Indium-111 (In)-labeled liposomes containing different ratios of DSPG were developed with a high labeling efficiency. In-labeled liposomes with higher DSPG content showed higher uptake by macrophage-like RAW264 cells. A biodistribution study demonstrated rapid blood clearance and selective accumulation in the liver and spleen, especially in normal mice injected with In-labeled liposomes with higher DSPG content. Accumulation in atherosclerotic plaques was evaluated using In-labeled DSPG liposomes, which had the highest DSPG content among the studied liposomes. In-labeled DSPG liposomes accumulated in the plaques and the radioactive regions were mostly consistent with the distribution of macrophages. The target-to-non-target ratio of In-labeled DSPG liposomes was higher than that of In-labeled control liposomes without DSPG. These results suggest that In-labeled liposomes containing DSPG are useful for nuclear medical diagnosis of atherosclerotic plaques.
巨噬细胞浸润是动脉粥样硬化斑块进展的一个特征性表现。由于含有1,2-二硬脂酰-sn-甘油-3-磷酸甘油(DSPG)的脂质体能够被巨噬细胞有效吞噬,我们推测含有DSPG的放射性标记脂质体可能可用于易损动脉粥样硬化斑块的核成像。我们制备了含有不同比例DSPG且标记效率高的铟-111(In)标记脂质体。DSPG含量较高的In标记脂质体在巨噬细胞样RAW264细胞中的摄取量更高。一项生物分布研究表明,在血液中清除迅速,且在肝脏和脾脏中选择性蓄积,尤其是在注射了DSPG含量较高的In标记脂质体的正常小鼠中。使用所研究脂质体中DSPG含量最高的In标记DSPG脂质体评估其在动脉粥样硬化斑块中的蓄积情况。In标记DSPG脂质体在斑块中蓄积,且放射性区域大多与巨噬细胞分布一致。In标记DSPG脂质体的靶与非靶比值高于不含DSPG的In标记对照脂质体。这些结果表明,含有DSPG的In标记脂质体可用于动脉粥样硬化斑块的核医学诊断。
J Nucl Med. 2013-12-12
Biomed Pharmacother. 2018-11-29