DSPE-PEG-COOH磷脂用于制备DSPE-PEG-DOX脂质体的相关文献（含合成路线）

DSPE-PEG-COOH用于制备DSPE-PEG-DOX的相关文献（含合成路线）

文献名: Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis

作者：

Taewon Hwang 1, Hee Dong Han, Chung Kil Song, Hasoo Seong, Jung Hyun Kim, Xiaoyuan Chen, Byung Cheol Shin

摘要：

抗癌药物的肿瘤特异性递送是药物开发过程中面临的主要挑战之一。在这项研究中，我们通过将新合成的DSPE-PEG2000-DOX（DPD）作为脂质成分掺入脂质体中制备了阿霉素（DOX）偶联脂质体（DCL），并测试了其体内抗肿瘤活性。通过酰胺键将DOX偶联到DSPE-PEG2000-COOH上合成了DPD，并通过（1）H-NMR分析确认了所得DPD的化学结构。通过薄膜浇铸水合法制备了脂质体尺寸为130nm的DCL。流式细胞术分析证实，DCL的细胞摄取明显高于传统脂质体。DCL对小鼠B16F10黑色素瘤荷瘤小鼠的抗肿瘤活性表明，DCL比传统脂质体更有效地抑制肿瘤生长，这可能是由于DOX介导的内吞过程。

实验使用方法:

Synthesis ofConjugate (SDSSD-DSPE)

A lipid-PEG-peptide combination that may subsequently be added to liposomes forbone targeting was developed, SDSSD was conjugated to DSPE-PEG2000-C00H usingcarbodiimide chemistry, based on the previously described method by Wang et al. withmodi fications [32. Briefly, DSPE-PEG2000-COOH was dissolved in 0.1 M MES bufferat pH 6.0 and stirred at 2-8 °C for 10 min. Then, EDC.HCl and NHS (20 equivalentseach) were added to the reaction mixture and stirred for 60 min at 2-8 °C. A 7.4 pHadjustment was made to the reaction mixture, Finally, SDSSD, previously dissolved inMilli-Q water, was added to the reaction mixture and stirred overnight. The resultantmixture was dialyzed using a 2KD dialysis membrane for 48 h to remove unconjugatedSDSSD. Purifield SDSSD-DSPE (conjugate) was freeze-dried and characterized by'H-NMRMaldi-TOF, and a Scanning Electron Microscope (SEM) followed by Energy Dispersive。

反应结构路线

重要检测:

文献核磁

重要实验结果说明

Synthesis of DSPE-PEG2000-DOX (DPD)Covalent conjugation of DOX to DSPE.PEG2000-COOH was confirmed by HNMR (500 MHz, Auto Sampler-HRMAS.FT-NMR, Bruker, Switzerland) analysis ofDPD. 'HNMR spectra were obtained forcomb polymer solutions in deuteratedchloroform. As shown in a Figure 3, theproton peaks of DOX (1,2 and 3)andDSPE-PEG2000-C00H(4 and 5)wereobserved at 7.4~8.2 ppm and 1.2~3.7ppm, respectively.