Enhanced localization of anticancer drug in tumor tissue using polyethylenimine-conjugated cationic liposomes

Hee Dong Han; Yeongseon Byeon; Hat Nim Jeon; Byung Cheol Shin

doi:10.1186/1556-276X-9-209

Enhanced localization of anticancer drug in tumor tissue using polyethylenimine-conjugated cationic liposomes

Nanoscale Res Lett. 2014 May 5;9(1):209. doi: 10.1186/1556-276X-9-209. eCollection 2014.

Authors

Hee Dong Han¹, Yeongseon Byeon¹, Hat Nim Jeon¹, Byung Cheol Shin²

Affiliations

¹ Department of Immunology, School of Medicine, Konkuk University, 268 Chungwondaero, Chungjusi, Chungcheongbukdo 380-701, South Korea.
² 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.

Abstract

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.

Keywords: Liposome; Localization; Polyethylenimine; Tumor.