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Updated: Mar 21, 2026

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Chitosan-based nanoparticles as drug delivery systems for doxorubicin: Optimization and modelling
Paula I P Soares1, Ana Isabel Sousa1, Jorge Carvalho Silva2
1i3N/CENIMAT, Department of Materials Science, Faculty of Science and Technology, Universidade NOVA de Lisboa, Campus de Caparica, 2829-516 Caparica, Portugal.
Doxorubicin was encapsulated into chitosan and O-HTCC nanoparticles for drug delivery. Doxorubicin release was higher in acidic conditions and showed a burst effect, indicating an anomalous release mechanism.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Nanotechnology
Background:
- Chitosan nanoparticles are widely explored for drug delivery due to their biocompatibility.
- Developing effective drug delivery systems for chemotherapeutics like doxorubicin is crucial for cancer treatment.
- Modifying chitosan, such as creating O-HTCC (ammonium-quaternary derivative of chitosan), can alter nanoparticle properties.
Purpose of the Study:
- To develop and characterize doxorubicin-loaded chitosan and O-HTCC nanoparticles.
- To investigate the doxorubicin release kinetics from these nanoparticles under different pH conditions.
- To evaluate the encapsulation efficiency and release mechanisms of the drug delivery systems.
Main Methods:
- Encapsulation of doxorubicin into chitosan and O-HTCC nanoparticles.
- Measurement of nanoparticle hydrodynamic diameter.
- In vitro doxorubicin release studies at acidic (pH 4.5) and physiological (pH 7.4) pH.
- Mathematical modeling of drug release kinetics.
Main Results:
- Nanoparticles with diameters below 200nm achieved high doxorubicin encapsulation (up to 70% for chitosan, 50% for O-HTCC).
- Doxorubicin release was significantly higher at acidic pH compared to physiological pH and was independent of chitosan molecular weight.
- O-HTCC nanoparticles exhibited a higher release rate than chitosan nanoparticles, with a burst release in the initial hours followed by a plateau after 24 hours.
Conclusions:
- Both chitosan and O-HTCC nanoparticles are effective systems for doxorubicin encapsulation and delivery.
- The acidic environment enhances doxorubicin release, suggesting potential for targeted delivery in tumor microenvironments.
- The release mechanism is primarily anomalous or mixed, consistent with chitosan's swelling behavior, and is influenced by pH.
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