Department of Immunology, School of Medicine, Konkuk University, 268 Chungwondaero, Chungjusi, Chungcheongbukdo 380-701, South Korea.
Research Center for Medicinal Chemistry, Division of Drug Discovery Research, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 305-600, South Korea.
Nanoscale Res Lett. 2014 May 5;9(1):209. doi: 10.1186/1556-276X-9-209. eCollection 2014.
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.
基于脂质体的药物传递系统在癌症治疗方面具有巨大的潜力。然而，为了增强有效载荷的定位，需要一种有效的方法将脂质体系统地递送到肿瘤组织中。在这项研究中，我们开发了由聚乙二亚胺（PEI）修饰的二硬脂酰基磷脂酰乙醇胺（DSPE）组成的阳离子脂质体，作为一种增强的局部药物传递系统。DSPE-PEI 脂质体的粒径为 130±10nm，通过将阳离子 PEI 掺入脂质体膜中，脂质体的 zeta 电位从-25mV 增加到 30mV。肿瘤细胞对 DSPE-PEI 脂质体的细胞内摄取比 DSPE 脂质体高 14 倍。在荷瘤小鼠肿瘤内注射脂质体后，DSPE-PEI 脂质体在肿瘤组织中的定位更高且持续，与 DSPE 脂质体相比。综上所述，我们的研究结果表明，DSPE-PEI 脂质体有望通过肿瘤内注射成为有效的药物载体，用于增强抗癌药物在肿瘤组织中的细胞内摄取和定位。
