DSPE-PEG-GRGDS修飾脂質體在紫杉醇遞送中的應用研究

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

作者：趙慧，王堅成，羅春蕾，孫啟時，張強

摘要：

目的:本研究以甘氨酸-精氨酸-甘氨酸-天冬氨酸-絲氨酸(glycine-arginine- glycine-aspartic acid-serine,GRGDS)五肽修飾的脂質體作為*癌藥物.紫杉醇的載體,對其體外理化性質和細胞毒作用進行評覽價.

方法:采用化學偶聯合成 DSPE-PEG-GRGDS,以此作為導向性材料,采用薄膜分散法制備載紫杉醇的PEG修飾長循環脂質體(GRGDS-SSL-PTX),并對脂質體的 包封率,粒徑和體外釋放率等性質進行了考察,同時采用人卵巢癌SKOV-3細胞和人乳腺癌MCF-7細胞進行了體外細胞生長抑制的評價.結果:與普通紫杉 醇長循環脂質體(SSL-PTX)相比,本研究制備的紫杉醇主動靶向脂質體(GRGDS-SSL-PTX)的粒徑,包封率,載藥量,體外釋放及穩定性等理 化性質無顯著差異,包封率約為95%,平均粒徑為(115.5±2.2)和(117.5±1.3)nm.冰凍蝕刻透射電鏡觀察結果表明,脂質體外觀基本圓 整且均勻分散.

體外釋放結果表明,12 h內分別有67.9%和72.3%的PTX從SSL-PTX和GRGDS-SSL-PTX中釋放.體外細胞毒實驗結果表明,GRGDS-SSL-PTX對 人卵巢癌SKOV-3細胞和人乳腺癌MCF-7細胞的生長抑制作用均有增強,分別為SSL-PTX的1.42倍和2.12倍.結論:GRGDS五肽修飾的 紫杉醇靶向脂質體成功制備,將有利于體內*的靶向*效果.

譯文：

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

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