Schroeder Avi, Sigal Alex, Turjeman Keren, Barenholz Yechezkel
Laboratory of Liposome and Membrane Research, Department of Biochemistry, Hebrew University-Hadassah Medical School, Jerusalem, Israel.
J Drug Target. 2008 Aug;16(7):591-5. doi: 10.1080/10611860802228939.
The ability of nano (approximately 100 nm) sterically stabilized liposomes (nSSLs) to target tissue invaded by a foreign body was demonstrated. Radioactively labeled nSSL remote loaded with the anti-inflammatory drug methylprednisolone hemisuccinate (MPS), to form nSSL-MPS, were injected i.v. to mice that, 2 or 3 weeks earlier, had either a thorn or a needle implanted in a hind leg. Twenty-four hours post-nSSL-MPS injection, animals were sacrificed, and the level of liposomes in the vicinity of the foreign body, in comparison to the tissue in the contralateral (normal) leg, was measured. The level of liposomes in the tissue surrounding the foreign body was twice as high as the level of liposomes found in the normal leg. Furthermore, the level of liposomes in the normal leg was similar to the level of liposomes measured in the legs of control animals that did not have an implanted foreign body and were treated with nSSL-MPS. The implications of these findings and the clinical applications of liposomal targeting are discussed.
已证实纳米级(约100纳米)空间稳定脂质体(nSSL)靶向异物侵入组织的能力。将负载有抗炎药物半琥珀酸甲泼尼龙(MPS)的放射性标记的nSSL远程加载形成nSSL-MPS,经静脉注射到2或3周前在后腿植入了刺或针的小鼠体内。注射nSSL-MPS 24小时后,处死动物,测量异物附近脂质体的水平,并与对侧(正常)腿的组织进行比较。异物周围组织中脂质体的水平是正常腿中脂质体水平的两倍。此外,正常腿中脂质体的水平与未植入异物并用nSSL-MPS治疗的对照动物腿中测量的脂质体水平相似。讨论了这些发现的意义以及脂质体靶向的临床应用。