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Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
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Smart sarcosinate-based catanionic vesicles for efficient doxorubicin delivery in tumor microenvironments
Rui L Machado1,2, Isabel S Oliveira1, Karenina Santos1,2
1CIQUP, IMS, Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto, 4169-007 Porto, Portugal. isabel.oliveira@fc.up.pt.
Nanoscale
|November 5, 2025
Summary
New pH-sensitive catanionic vesicles show promise for cancer therapy. These biocompatible nanocarriers efficiently deliver drugs like doxorubicin (DOX) to cancer cells, enhancing efficacy and reducing toxicity at low doses.
Area of Science:
- Materials Science
- Nanotechnology
- Biomedical Engineering
Background:
- Catanionic mixtures form self-assembled aggregates with tunable properties, offering potential for drug delivery.
- Existing catanionic vesicles often lack favorable cytotoxicity, high drug loading, and bioactivity.
- Developing biocompatible and effective nanocarriers for chemotherapy remains a significant challenge.
Purpose of the Study:
- To systematically investigate pH-sensitive catanionic vesicles for drug delivery applications.
- To evaluate the cytotoxicity, drug loading, and release profiles of novel vesicle formulations.
- To assess the *in vitro* efficacy of drug-loaded vesicles in cancer cells.
Main Methods:
- Formulation of catanionic vesicles using sodium lauroyl sarcosinate (SLSar) and cationic double-tailed surfactants.
- Characterization of vesicle properties including size, surface charge, and colloidal stability.
- Cytotoxicity screening using L929 fibroblasts and doxorubicin (DOX) encapsulation and release studies.
Main Results:
- Spontaneous formation of stable vesicles at low critical aggregation concentrations.
- Gemini/SLSar systems demonstrated superior DOX encapsulation efficiency and pH-sensitive release at acidic pH.
- Rapid cellular uptake and potent cytotoxicity of DOX-loaded vesicles at significantly lower concentrations than free DOX.
Conclusions:
- SLSar-based catanionic vesicles represent a simple, stable, and tunable platform for drug delivery.
- These vesicles show significant potential for pH-responsive, low-dose cancer chemotherapy.
- The enhanced therapeutic efficacy suggests potential for reduced systemic toxicity in cancer treatment.
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