Preparation and characterization of zedoary turmeric oil–loaded insulin-modified sterically stabilized liposomes

Abstract

The poor selectivity of anticancer drugs often leads to their multiplicate dose-limiting toxicities in humans, which severely restricts their clinical application. In this study, a novel liposomal formulation of zedoary turmeric oil (ZTO) targeting the insulin receptor (IR) was prepared by covalently conjugating insulin to the terminal of the polyethylene glycol (PEG) chain of sterically stabilized liposomes. In vitro assays indicated that a higher uptake of insulin-modified sterically stabilized liposomes (ISSLs) was observed in SMMC-7721 hepatocarcinoma cells overexpressing insulin receptors. IC₅₀ values of ISSLs, NTLs (nontargeted liposomes), and ZTO injection (free ZTO) against SMMC-7721, determined by MTT assays, were 157.2, 256.7, and 43.3 μg·ml⁻¹, respectively. Plasma-clearance profiles of ZTO in the liposomal formulations were then compared with that of ZTO injection. The liposomal formulations showed much longer terminal half-lives (11.24 and 14.73 hours for ISSLs and NTLs, respectively) than that of ZTO injection (1.45 hours). All results above indicated the ISSLs were potentially useful for the treatment of IR (+) tumors and are worthy of further investigation.

Keywords::

• Liposomes
• insulin receptor
• targeted drug delivery
• cancer

Acknowledgment

This work was surported by the Science and Technology Project of Education Department of Jiangxi Province, China (grant no. GJJ08393).

Declaration of interest: The authors report no financial conflicts of interest. The authors alone are responsible for the content and writing of this paper.