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Updated: Dec 9, 2025

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Tumor Microenvironmental Responsive Liposomes Simultaneously Encapsulating Biological and Chemotherapeutic Drugs for
Liang Kong1, Shi-Meng Zhang2, Jia-Hao Chu3
1School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian 116600, People's Republic of China.
Background:
Non-small cell lung cancer (NSCLC) is one of the most lethal types of cancer with highly infiltrating. Chemotherapy is far from satisfactory, vasculogenic mimicry (VM) and angiogenesis results in invasion, migration and relapse.
Purpose:
The objective of this study was to construct a novel CPP (mmp) modified vinorelbine and dioscin liposomes by two new functional materials, DSPE-PEG2000-MAL and CPP-PVGLIG-PEG5000, to destroy VM channels, angiogenesis, EMT and inhibit invasion and migration.
Methods And Results:
The targeting liposomes could be enriched in tumor sites through passive targeting, and the positively charged CPP was exposed and enhanced active targeting via electrostatic adsorption after being hydrolyzed by MMP2 enzymes overexpressed in the tumor microenvironment. We found that CPP (mmp) modified vinorelbine and dioscin liposomes with the ideal physicochemical properties and exhibited enhanced cellular uptake. In vitro and in vivo results showed that CPP (mmp) modified vinorelbine and dioscin liposomes could inhibit migration and invasion of A549 cells, destroy VM channels formation and angiogenesis, and block the EMT process. Pharmacodynamic studies showed that the targeting liposomes had obvious accumulations in tumor sites and magnificent antitumor efficiency.
Conclusion:
CPP (mmp) modified vinorelbine plus dioscin liposomes could provide a new strategy for NSCLC.
Insights
This study developed novel CPP(mmp) modified liposomes carrying vinorelbine and dioscin. These liposomes effectively target non-small cell lung cancer (NSCLC) tumors, inhibiting invasion, migration, and tumor growth.
Area of Science:
- Oncology
- Nanomedicine
- Drug Delivery
Background:
- Non-small cell lung cancer (NSCLC) presents significant challenges due to its invasive nature.
- Current chemotherapy for NSCLC is often inadequate, with vasculogenic mimicry (VM) and angiogenesis contributing to metastasis and recurrence.
Purpose of the Study:
- To create novel CPP(mmp) modified liposomes encapsulating vinorelbine and dioscin.
- To target and disrupt VM channels, angiogenesis, and epithelial-mesenchymal transition (EMT) in NSCLC.
- To inhibit cancer cell invasion and migration.
Main Methods:
- Liposomes were functionalized with DSPE-PEG2000-MAL and CPP-PVGLIG-PEG5000 for enhanced targeting.
- CPP(mmp) moiety was designed for MMP2-triggered active targeting in the tumor microenvironment.
- In vitro and in vivo studies evaluated liposome physicochemical properties, cellular uptake, anti-migration, anti-invasion, anti-angiogenesis, and anti-VM efficacy.
Main Results:
- Targeting liposomes demonstrated passive accumulation in tumors and active targeting via CPP(mmp) exposure.
- Enhanced cellular uptake and ideal physicochemical properties were observed.
- Significant inhibition of A549 cell migration and invasion, VM, angiogenesis, and EMT was achieved.
- In vivo studies confirmed tumor site accumulation and potent antitumor effects.
Conclusions:
- CPP(mmp) modified vinorelbine and dioscin liposomes represent a promising new therapeutic strategy for NSCLC.
- This approach offers a novel method to combat NSCLC progression by targeting key pathological processes.
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