DSPE-PEG-GRGDS修饰脂质体在紫杉醇递送中的应用研究

链接：https://xueshu.baidu.com/usercenter/paper/show?paperid=22a90749392dd40393a64f063e5f4c0f&site=xueshu_se

作者：赵慧，王坚成，罗春蕾，孙启时，张强

摘要：

目的:本研究以甘氨酸-精氨酸-甘氨酸-天冬氨酸-丝氨酸(glycine-arginine- glycine-aspartic acid-serine,GRGDS)五肽修饰的脂质体作为*癌药物.紫杉醇的载体,对其体外理化性质和细胞毒作用进行评览价.

方法:采用化学偶联合成 DSPE-PEG-GRGDS,以此作为导向性材料,采用薄膜分散法制备载紫杉醇的PEG修饰长循环脂质体(GRGDS-SSL-PTX),并对脂质体的 包封率,粒径和体外释放率等性质进行了考察,同时采用人卵巢癌SKOV-3细胞和人乳腺癌MCF-7细胞进行了体外细胞生长抑制的评价.结果:与普通紫杉 醇长循环脂质体(SSL-PTX)相比,本研究制备的紫杉醇主动靶向脂质体(GRGDS-SSL-PTX)的粒径,包封率,载药量,体外释放及稳定性等理 化性质无显著差异,包封率约为95%,平均粒径为(115.5±2.2)和(117.5±1.3)nm.冰冻蚀刻透射电镜观察结果表明,脂质体外观基本圆 整且均匀分散.

体外释放结果表明,12 h内分别有67.9%和72.3%的PTX从SSL-PTX和GRGDS-SSL-PTX中释放.体外细胞毒实验结果表明,GRGDS-SSL-PTX对 人卵巢癌SKOV-3细胞和人乳腺癌MCF-7细胞的生长抑制作用均有增强,分别为SSL-PTX的1.42倍和2.12倍.结论:GRGDS五肽修饰的 紫杉醇靶向脂质体成功制备,将有利于体内*的靶向*效果.

译文：

Objective: This study used glycine arginine glycine aspartic acid serine (GRGDS) pentapeptide modified liposomes as anticancer drugs Evaluate the in vitro physicochemical properties and cytotoxicity of paclitaxel as a carrier Methods: The chemical coupling synthesis of DSPE-PEG-GRGDS was used as the guiding material, and the paclitaxel loaded PEG modified long-cycle liposomes (GRGDS-SSL-PTX) were prepared by the film dispersion method. The encapsulation efficiency, particle size and in vitro release rate of the liposomes were investigated. At the same time, the cell growth inhibition of human ovarian cancer SKOV-3 cells and human breast cancer MCF-7 cells were evaluated in vitro Result: Compared with conventional paclitaxel long circulating liposomes (SSL-PTX), the paclitaxel actively targeted liposomes (GRGDS-SSL-PTX) prepared in this study showed no significant differences in particle size, encapsulation efficiency, drug loading, in vitro release, and stability. The encapsulation efficiency was about 95%, and the average particle size was (115.5 ± 2.2) and (117.5 ± 1.3) nm. The observation results of cryoetched transmission electron microscopy showed that the appearance of the liposomes was basically round and uniformly dispersed The in vitro release results showed that 67.9% and 72.3% of PTX were released from SSL-PTX and GRGDS-SSL-PTX, respectively, within 12 hours The cytotoxicity test in vitro showed that GRGDS-SSL-PTX enhanced the growth inhibition of human ovarian cancer SKOV-3 cells and human breast cancer MCF-7 cells, which were 1.42 times and 2.12 times higher than SSL-PTX, respectively Conclusion: The successful preparation of paclitaxel targeted liposomes modified with GRGDS pentapeptide will be beneficial for the targeted therapy of tumors in vivo

DOI：10.3321/j.issn:1003-3734.2008.23.010

西安齐岳生物提供相关产品：

DSPE-PEG-cisplatin

DSPE-PEG-CLS

DSPE-PEG-COOH CAS No.: 1403744-37-5

DSPE-PEG-Cyanur

DSPE-PEG-DA

DSPE-PEG-Dopamine

DSPE-PEG-DOTA

DSPE-PEG-Estrogen

DSPE-PEG-Galactose

DSPE-PEG-Glucose

DSPE-PEG-Glutamic acid

DSPE-PEG-Glycine triarginine

以上文章内容来源各类期刊或文献，如有侵权请联系我们删除！