DSPE-PEI助力构建高电位、强定位性的脂质体系统

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

作者：韩熙东，边永善，帽子·尼姆·杰恩，申秉哲

摘要：基于脂质体的药物递送系统在癌症*中拥有巨大的潜力。然而，为了增强有效载荷的定位，需要一种有效的脂质体系统性递送至*组织的方法。本研究开发了由聚乙烯亚胺 (PEI) 共轭二硬脂酰甘油磷酸乙醇胺 (DSPE) 组成的阳离子脂质体，作为一种增强的局部药物递送系统。DSPE-PEI 脂质体的粒径为 130 ± 10 nm，通过将阳离子 PEI 引入脂质体膜，脂质体的 zeta 电位从 -25 mV 提高至 30 mV。*细胞对 DSPE-PEI 脂质体的细胞内摄取率比 DSPE 脂质体高 14 倍。将脂质体注射到荷瘤小鼠体内后，与DSPE脂质体相比，DSPE-PEI脂质体在*组织中表现出更高且更持久的定位。综上所述，我们的研究结果表明，DSPE-PEI脂质体有望成为一种有效的药物载体，通过*内注射增强*癌药物在*组织中的细胞摄取和定位。

译文：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.

西安齐岳生物提供相关产品：

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

DSPE-PEG-MPG（二硬脂酰基磷脂酰乙醇胺-聚乙二醇-PH响应性细胞穿膜肽)

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

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

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

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