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.
Highlights
Liposome-based approaches, which show great potential for cancer therapy, allow for the development of a broad armamentarium of targeted drugs [1,2,3]
Intratumoral injection is an effective method for liposomemediated drug delivery into tumor tissues
The use of DOX-loaded DSPE-PEI cationic liposomes was found to result in significantly increased in vitro intracellular uptake compared with control liposomes
Summary
Liposome-based approaches, which show great potential for cancer therapy, allow for the development of a broad armamentarium of targeted drugs [1,2,3]. One of the key challenges in the application of liposomal drug delivery for chemotherapy is the requirement of efficient drug localization in tumor tissue. These liposomal systems are normally injected intravenously for systemic application. Drug delivery systems formulated to deliver high concentration of drugs over an extended period could be an ideal strategy to maximize the therapeutic benefit and avoid possible side effects [7]. Because low molecular weight drugs can rapidly pass into the bloodstream after intratumoral injection and because the retention time of such drugs in tumors is considerably short, new strategies to enhance the drug delivery and therapeutic effects in tumor tissues are needed
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