论文参考文献：Ligation Strategies for Targeting Liposomal Nanocarriers小说作者：Patricia Marqués-Gallego, Anton I. P. M. de Kroon论文参考文献联接：//onlinelibrary.wiley.com/doi/full/10.1155/2014/129458提要：Two different approaches with two different anisamide derivatives were described for conjugating the targeting ligand to the DSPE-PEG-amine phospholipid. In the first approach, 7-[2-(4-methoxybenzylamino)-ethylamino]heptanoic acid was conjugated to the DSPE-PEG-amine lipid using standard DCC/DMAP chemistry for amine-carboxyl conjugation. The second approach yielded the N-alkylated lipid using an N-(2-bromoethyl)-4-methoxybenzamide derivative and DSPE-PEG-amine. The authors showed that the synthesis of the anisamide-lipid by the second approach has 10-fold greater yield than the standard amine-carboxyl coupling. The anisamide-lipid was mixed with the other lipids (POPC and cholesterol) at the desired concentration to form liposomes in citrate buffer (pH 4.0). Controlling the amount of targeting ligand included in the liposomes is an additional advantage of this approach. Doxorubicin was then loaded into the liposomes using the transmembrane pH gradient (acidic inside) according to the remote loading technique developed by Mayer et al. [54]. The formulation showed promising results in the in vivo treatment of DU-145 tumors in nude mice. The partitioning of the ligated lipid between the exterior and the interior of the liposome upon liposome formation must be considered, with an estimated 50% of the targeting ligand entrapped in the inner side of the bilayer. Positive results obtained in in vitro studies targeting sigma receptors suggested sufficient targeting ligand on the outer side of the liposome bilayer. Possible leakage of doxorubicin from the liposomes induced by the presence of the ligand was not examined.

说明了用2种不相同的茴香酰胺衍化物将靶向药物配体偶联到DSPE-PEG胺磷脂的2种不相同方式方法。在第一点种的策略中，用到规则DCC/DMAP化学上的的策略将7-[2-（4-甲氧基苄氨基）-乙基氨基]庚酸偶联到DSPE-PEG胺脂质上，在胺羧基偶联。第三种的方式使用的N-（2-溴乙基）-4-甲氧基苯甲酰胺繁衍物和DSPE-PEG胺引起N-烷基化脂质。我得出结论，依据第三种的方式组成茴香酰胺脂质的产出率比要求胺羧基偶联高10倍。将茴香酰胺脂质与别的脂质（POPC和胆固）以必需含量混合型，在柚子酸盐缓存液（pH 4.0）中建立脂质体。控住脂质体中包涵的靶向药物配体的量是这一手段的另一类个益处。再基于Mayer宋江因设计规划的即远程初始化的技术，在使用跨膜pH梯度方向（内外部呈含酸性）将阿霉素初始化到脂质体中。该药制剂在裸鼠身体内疗法DU-145癌肿的方面显现出有愿的毕竟。需要满足脂质体态成时连入的脂质在脂质身休外部和内部的两者的配置，预计50%的靶向药物疗法配体包埋在单层的后侧。在针对于sigma感觉的身休外探析中获取的弱阳结论体现了，脂质体单层后侧有已经可以的靶向药物疗法配体。未进行检查配体发生诱发阿霉素从脂质体中渗漏的几率性。有关系网友推荐：DSPE-PEG-c(RGDfk)DSPE-PEG-c(RGDfK)-FITCDSPE-PEG-c(RGDfK)-BiotinDSPE-PEG-c(RGDfc)DSPE-PEG-GE11DSPE-PEG-PTPDSPE-PEG-T7(HAIYPRH)DSPE-PEG-THDSPE-PEG-YIGSRDSPE-PEG-NGRDSPE-PEG-Angiopep-2以下篇文章主要内容原因常见期刊杂志或文章，以免侵犯商标权请保持联系你们误删！