Promising positive liver targeting delivery system based on arabinogalactan-anchored polymeric micelles of norcantharidin
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Updated: Feb 2, 2026

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Published on: June 8, 2016
Zhenghai Zhang1,2, Lei Yang1,2, Jian Hou1,2
1a Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese Medicine , Nanjing , China.
Abstract:
Liver cancer is the third most common cause of global cancer-related deaths. This study focused on newly developed drug delivery systems with hepatocyte asialoglycoprotein receptor binding targeting the liver. Although norcantharidin (NCTD) is effective in primary liver cancer treatment, its toxicity in the urinary system remains. Positive liver-targeting effect could be achieved by preparing polymer micelles by arabinogalactan on the surface of N-(4-methylimidazole)-hydroxyethyl-chitosan (MHC). HepG2 cells were used to analyze the cytotoxicity, invasion, apoptosis and uptake of NCTD-loaded micelles. The in vivo antitumor efficacy of NCTD-M was evaluated using tumor-bearing nude mice. Successful preparation of NCTD-M was shown. In vivo imaging showed that micelles significantly increased positive liver drug targeting. Laser confocal microscopy showed increased cellular uptake of micelles. NCTD-M also enhanced cell invasion and the proportion of apoptotic cells. Compared with the other groups, the micelles showed better antitumor effects in vivo. Therefore, the positive liver-targeting NCTD-M, which can enhance antitumor efficacy and reduce toxicity, could be a promising and effective therapeutic agent for liver cancer treatment.
Insights
This study developed novel liver-targeting micelles loaded with norcantharidin (NCTD) to treat liver cancer. These micelles enhance drug delivery to the liver, improving antitumor efficacy and reducing toxicity.
Area of Science:
- Oncology
- Materials Science
- Pharmacology
Background:
- Liver cancer is a leading cause of cancer mortality worldwide.
- Norcantharidin (NCTD) shows efficacy against primary liver cancer but has urinary system toxicity.
- Targeted drug delivery systems are needed to improve liver cancer treatment and reduce side effects.
Purpose of the Study:
- To develop and evaluate novel polymer micelles for targeted liver drug delivery.
- To investigate the efficacy of NCTD-loaded micelles (NCTD-M) for liver cancer treatment.
- To assess the potential of NCTD-M to enhance antitumor activity and reduce systemic toxicity.
Main Methods:
- Preparation of arabinogalactan-coated N-(4-methylimidazole)-hydroxyethyl-chitosan (MHC) polymer micelles loaded with NCTD.
- In vitro studies using HepG2 cells to analyze cytotoxicity, invasion, apoptosis, and cellular uptake.
- In vivo evaluation of NCTD-M antitumor efficacy in tumor-bearing nude mice using imaging and efficacy studies.
Main Results:
- Successfully prepared NCTD-loaded MHC micelles (NCTD-M) with positive liver-targeting capabilities.
- In vivo imaging confirmed enhanced drug accumulation in the liver.
- In vitro and in vivo studies demonstrated increased cellular uptake, enhanced cell invasion, elevated apoptosis, and superior antitumor effects of NCTD-M compared to controls.
Conclusions:
- The developed liver-targeting NCTD-M effectively deliver drugs to the liver, enhancing antitumor efficacy.
- NCTD-M show potential for reducing toxicity associated with NCTD treatment.
- This targeted drug delivery system represents a promising therapeutic strategy for liver cancer.
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