医学文献：Ligation Strategies for Targeting Liposomal Nanocarriers我们：Patricia Marqués-Gallego, Anton I. P. M. de Kroon文章外链：//onlinelibrary.wiley.com/doi/full/10.1155/2014/129458引言：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.

描述英文了用哪几种不相同的茴香酰胺衍生物物将靶向疗法配体偶联到DSPE-PEG胺磷脂的哪几种不相同办法。在第一名种策略中，便用标准DCC/DMAP化学工业策略将7-[2-（4-甲氧基苄氨基）-乙基氨基]庚酸偶联到DSPE-PEG胺脂质上，使用在胺羧基偶联。其次种策略运行N-（2-溴乙基）-4-甲氧基苯甲酰胺衍生产品物和DSPE-PEG胺带来N-烷基化脂质。作家揭示，实现其次种策略分解成茴香酰胺脂质的产出率比标准规定胺羧基偶联高10倍。将茴香酰胺脂质与任何脂质（POPC和低密度胆固醇）以所需要的浓硫酸浓度混合着，在柠檬汁酸盐缓冲器液（pH 4.0）中转变成脂质体。管理脂质体中包涵的靶向药物配体的量是类似这些的方式的另一个说的是个优点有哪些。接下来依照Mayer等等开放的手机远程读取新技术，食用跨膜pH梯度方向（内控呈呈酸性）将阿霉素读取到脂质体中。该溶液剂在裸鼠胃中缓解DU-145肉瘤角度彰显出有渴望的结杲。要确定脂质身材成时连入的脂质在脂质休外部和內部两者的左右，加权平均值50%的靶点配体包埋在加厚的里侧。在真对sigma感觉的休外实验中取得的抗体阳性结局说明，脂质体加厚两侧有充足的靶点配体。未进行检查配体留存诱导型阿霉素从脂质体中漏粪的很有机率。相关内容比较适合：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上面好的文章內容收入各样论文期刊或论文资料，见谅侵权商标请联络咱们全部删除！