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Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes
Published on: July 30, 2020
Preparation and characterization of zedoary turmeric oil-loaded insulin-modified sterically stabilized liposomes
Zhiwen Yang1, Dahua Fu, Liang Zhu
1Department of Pharmaceutical Sciences, Gannan Medical College, Ganzhou, China. menghua001@sina.com
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. IC(50) 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 microg x 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.
Insights
This study developed novel liposomes targeting insulin receptors (IR) for cancer treatment. These targeted liposomes showed improved drug delivery and longer circulation times, offering potential for IR-positive tumors.
Area of Science:
- Pharmacology
- Nanotechnology
- Oncology
Background:
- Anticancer drugs often exhibit poor selectivity, causing dose-limiting toxicities and limiting clinical use.
- Targeting specific receptors on cancer cells can improve drug efficacy and reduce side effects.
Purpose of the Study:
- To develop a novel liposomal formulation of zedoary turmeric oil (ZTO) that targets the insulin receptor (IR).
- To evaluate the in vitro and pharmacokinetic properties of the targeted liposomes.
Main Methods:
- Covalently conjugating insulin to polyethylene glycol (PEG) chains of liposomes to create insulin-modified sterically stabilized liposomes (ISSLs).
- Assessing cellular uptake in SMMC-7721 hepatocarcinoma cells overexpressing IR.
- Determining IC(50) values using MTT assays.
- Comparing plasma-clearance profiles and terminal half-lives of liposomal formulations versus free ZTO.
Main Results:
- ISSLs demonstrated higher uptake in IR-overexpressing SMMC-7721 cells compared to non-targeted liposomes.
- IC(50) values indicated greater efficacy of ISSLs against SMMC-7721 cells (157.2 μg/mL) than non-targeted liposomes (256.7 μg/mL) and free ZTO (43.3 μg/mL).
- Liposomal formulations exhibited significantly longer terminal half-lives (11.24-14.73 hours) than free ZTO (1.45 hours).
Conclusions:
- The developed ISSLs show potential for treating IR-positive tumors due to enhanced cellular uptake and improved pharmacokinetic profiles.
- Further investigation is warranted to explore the therapeutic efficacy of ISSLs in preclinical and clinical settings.
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