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Solid-State Formation of a Potential Melphalan Delivery Nanosystem Based on β-Cyclodextrin and Silver Nanoparticles
Rodrigo Sierpe1,2,3, Orlando Donoso-González1,2,4,5, Erika Lang1
1Departamento de Química, Facultad de Ciencias, Universidad de Chile, Las Palmeras #3425, Ñuñoa, Santiago 7800003, Chile.
International Journal of Molecular Sciences
|February 25, 2023
Summary
This study developed a novel nanocarrier using beta-cyclodextrin (βCD) and silver nanoparticles (AgNPs) to improve melphalan (Mel) delivery for cancer therapy. The resulting βCD-Mel-AgNPs system enhances Mel
Area of Science:
- Nanotechnology
- Materials Science
- Pharmacology
Background:
- Melphalan (Mel) is an antineoplastic drug with limited efficacy due to poor solubility, rapid hydrolysis, and non-specificity.
- Beta-cyclodextrin (βCD) can enhance drug solubility and stability.
- Silver nanoparticles (AgNPs) offer unique properties for drug delivery systems.
Purpose of the Study:
- To develop a novel nanocarrier system for melphalan (Mel) using β-cyclodextrin (βCD) and silver nanoparticles (AgNPs).
- To characterize the physicochemical properties of the βCD-Mel-AgNPs complex.
- To evaluate the in vitro permeability and potential of the nanosystem for cancer therapy.
Main Methods:
- Formation of a βCD-Mel complex followed by deposition of AgNPs via magnetron sputtering.
- Characterization using techniques to determine loading capacity, association constant, and degree of solubilization.
- Analysis of nanoparticle size, dissolution properties, and in vitro permeability assays.
Main Results:
- The βCD-Mel-AgNPs system demonstrated a loading capacity of 27% and an association constant of 625 M⁻¹.
- Solid-state AgNPs averaged 15 ± 3 nm, stabilized by Mel's functional groups.
- Dissolution yielded a colloidal solution with a hydrodynamic diameter of 116 nm and enhanced Mel permeability.
Conclusions:
- The developed βCD-Mel-AgNPs nanosystem effectively enhances melphalan's solubility, stability, and permeability.
- This novel nanocarrier shows significant promise for improving melphalan's therapeutic performance in cancer treatment.
- Further research is warranted to explore its full potential in preclinical and clinical cancer therapy.

