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Galactose-Containing Polymer-DOX Conjugates for Targeting Drug Delivery
Yujie Sun1, Jing Zhang1, Jian Han2
1School of Pharmacy, Binzhou Medical University, 346 Guanhai Road, Yantai, 264003, People's Republic of China.
AAPS Pharmscitech
|June 12, 2016
Summary
A new drug delivery system using galactose-based polymers conjugated with doxorubicin (DOX) shows pH-responsive release and targets liver cancer cells (HepG2) via ASGP receptors, enhancing anticancer efficacy.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Drug Delivery Systems
Background:
- Developing targeted drug delivery systems is crucial for improving cancer therapy efficacy and reducing side effects.
- Galactose-based polymers offer potential for targeted delivery due to specific receptor interactions on cancer cells.
- Doxorubicin (DOX) is a potent chemotherapeutic agent with limitations in targeted delivery.
Purpose of the Study:
- To fabricate and characterize a novel multifunctional drug delivery system for targeted hepatoma therapy.
- To evaluate the pH-responsive drug release and cellular uptake of the novel nanoparticles.
- To assess the in vitro anticancer efficacy of the targeted drug delivery system.
Main Methods:
- Conjugation of methoxy-poly(ethylene glycol)-block-poly(6-O-methacryloyl-D-galactopyranose) (mPEG-b-PMAGP) with doxorubicin (DOX) via an acid-labile linkage.
- Characterization of nanoparticle size and morphology using Dynamic Light Scattering (DLS) and Transmission Electron Microscopy (TEM).
- In vitro drug release studies at different pH values, cellular uptake evaluation using Confocal Laser Scanning Microscopy (CLSM) and Flow Cytometry (FCM), and cytotoxicity assays.
Main Results:
- Spherical mPEG-b-PMAGP-co-DOX nanoparticles with a diameter of approximately 54.8 nm were successfully fabricated.
- DOX release from nanoparticles demonstrated pH-responsiveness, with higher release at lower pH.
- Enhanced cellular uptake and higher anticancer efficacy were observed in asialoglycoprotein (ASGP) receptor-positive HepG2 cells compared to ASGP receptor-negative MCF-7 and A549 cells.
Conclusions:
- The mPEG-b-PMAGP-co-DOX nanoparticles exhibit pH-responsive drug release and targeted delivery to hepatoma cells via ASGP receptor-mediated endocytosis.
- This novel multifunctional system shows significant potential as a targeted drug delivery platform for effective hepatoma therapy.
- The combination of targeting ligands and pH-sensitive release offers a promising strategy for improving chemotherapy outcomes.
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