DSPE-PEI助力構(gòu)建高電位、強(qiáng)定位性的脂質(zhì)體系統(tǒng)

鏈接：https://link.springer.com/article/10.1186/1556-276X-9-209

作者：韓熙東，邊永善，帽子·尼姆·杰恩，申秉哲

摘要：基于脂質(zhì)體的藥物遞送系統(tǒng)在癌癥*中擁有巨大的潛力。然而，為了增強(qiáng)有效載荷的定位，需要一種有效的脂質(zhì)體系統(tǒng)性遞送至*組織的方法。本研究開(kāi)發(fā)了由聚乙烯亞胺 (PEI) 共軛二硬脂酰甘油磷酸乙醇胺 (DSPE) 組成的陽(yáng)離子脂質(zhì)體，作為一種增強(qiáng)的局部藥物遞送系統(tǒng)。DSPE-PEI 脂質(zhì)體的粒徑為 130 ± 10 nm，通過(guò)將陽(yáng)離子 PEI 引入脂質(zhì)體膜，脂質(zhì)體的 zeta 電位從 -25 mV 提高至 30 mV。*細(xì)胞對(duì) DSPE-PEI 脂質(zhì)體的細(xì)胞內(nèi)攝取率比 DSPE 脂質(zhì)體高 14 倍。將脂質(zhì)體注射到荷瘤小鼠體內(nèi)后，與DSPE脂質(zhì)體相比，DSPE-PEI脂質(zhì)體在*組織中表現(xiàn)出更高且更持久的定位。綜上所述，我們的研究結(jié)果表明，DSPE-PEI脂質(zhì)體有望成為一種有效的藥物載體，通過(guò)*內(nèi)注射增強(qiáng)*癌藥物在*組織中的細(xì)胞攝取和定位。

譯文：Liposome-based drug delivery systems hold great potential for cancer therapy. However, to enhance the localization of payloads, an efficient method of systemic delivery of liposomes to tumor tissues is required. In this study, we developed cationic liposomes composed of polyethylenimine (PEI)-conjugated distearoylglycerophosphoethanolamine (DSPE) as an enhanced local drug delivery system. The particle size of DSPE-PEI liposomes was 130?±?10 nm and the zeta potential of liposomes was increased from -25 to 30 mV by the incorporation of cationic PEI onto the liposomal membrane. Intracellular uptake of DSPE-PEI liposomes by tumor cells was 14-fold higher than that of DSPE liposomes. After intratumoral injection of liposomes into tumor-bearing mice, DSPE-PEI liposomes showed higher and sustained localization in tumor tissue compared to DSPE liposomes. Taken together, our findings suggest that DSPE-PEI liposomes have the potential to be used as effective drug carriers for enhanced intracellular uptake and localization of anticancer drugs in tumor tissue through intratumoral injection.

西安pg電子官方生物提供相關(guān)產(chǎn)品：

DSPE-PEG-RGD(二硬脂酰基磷脂酰乙醇胺-聚乙二醇-整合素靶向環(huán)肽)

DSPE-PEG-MPG（二硬脂�；�磷脂酰乙醇胺-聚乙二醇-PH響應(yīng)性細(xì)胞穿膜肽)

DSPE-PEG-Trastuzumab（二硬脂�；�磷脂酰乙醇胺-聚乙二醇-*靶向蛋白)

DSPE-PEG-rhuMAb HER2-Fab’or scFv（二硬脂酰基磷脂酰乙醇胺-聚乙二醇-*靶向蛋白)

DSPE-PEG-YEQDPWGVKWWY（二硬脂�；�磷脂酰乙醇胺-聚乙二醇-*靶向蛋白)

DSPE-PEG-Antinucleosome mAb 2C5（二硬脂�；�磷脂酰乙醇胺-聚乙二醇-*靶向蛋白)

DSPE-PEG-OX26 mAb（二硬脂�；�磷脂酰乙醇胺-聚乙二醇-*靶向蛋白)

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