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Updated: Nov 10, 2025
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
A Combined Self-Assembled Drug Delivery for Effective Anti-Breast Cancer Therapy
Hairong Wang1, Yawen Zhang1, Xiangle Zeng1
1School of Pharmacy, Bengbu Medical College, Bengbu, 233030, People's Republic of China.
Aim:
The metastasis of breast cancer is an important cause of tumor recurrence. This study highlights that tyrosine kinase inhibitors dasatinib (DAS) and rosiglitazone (ROZ) inhibit tumor growth and reduce the occurrence of tumor cell metastasis. Due to the poor water solubility, short half-time in the body of DAS and ROZ, which increases the difficulty of tumor treatment, as well as the demand for nano-drug delivery systems for organ-specific therapies.
Methods:
Hyaluronic acid (HA) and DAS are bonded by a pH-sensitive ester bond to form an HA-DAS polymer. Then, ROZ was added as the core, D-A-tocopherol polydiethylene glycol isosuccinate (TPGS) and HA-DAS were used as carriers to form HA-DAS and TPGS mixed micelle system loaded with ROZ (THDR-NPs). The size and structure of THDR-NPs were characterized, the drug release, stability and biosafety of THDR-NPs were studied. In vitro, the cytotoxicity, targeting effect and tumor metastasis inhibition of THDR-NPs were evaluated in human breast cancer cell lines. In addition, the selective potency of designed THDR-NPs in depleting was further verified in vivo in the tumor-bearing nude mice model.
Results:
The designed THDR-NPs have a particle size of less than 100 nm, good stability, biological safety and sustained release, and showed strong therapeutic effects on breast cancer models in vitro and in vivo. Moreover, it has been proved that THDR-NPs have the ability to inhibit tumor metastasis.
Conclusion:
DAS and ROZ were designed into micelles, the efficacy of THDR-NPs was higher than that of free drugs. These results indicate that nanoparticles have a good application prospect in the treatment of tumor metastasis.
Insights
This study developed novel nanoparticles (THDR-NPs) to improve breast cancer treatment by enhancing drug delivery. The nanoparticles effectively inhibited tumor growth and metastasis in preclinical models.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Breast cancer metastasis is a major cause of recurrence.
- Existing drugs like dasatinib (DAS) and rosiglitazone (ROZ) show potential but suffer from poor solubility and short half-lives.
- There is a need for advanced nano-drug delivery systems for targeted cancer therapies.
Purpose of the Study:
- To develop a nanoparticle system (THDR-NPs) for improved delivery of dasatinib and rosiglitazone.
- To evaluate the efficacy of THDR-NPs in inhibiting breast cancer growth and metastasis.
- To assess the stability, safety, and targeting capabilities of the designed nanoparticles.
Main Methods:
- Formulated THDR-NPs using hyaluronic acid (HA), DAS, ROZ, and TPGS via a pH-sensitive ester bond.
- Characterized nanoparticle size, structure, drug release, stability, and biosafety.
- Evaluated in vitro cytotoxicity, targeting, and metastasis inhibition in breast cancer cell lines.
- Verified in vivo efficacy in tumor-bearing nude mice models.
Main Results:
- THDR-NPs exhibited a particle size under 100 nm with good stability, safety, and sustained drug release.
- The nanoparticles demonstrated significant therapeutic effects against breast cancer in both in vitro and in vivo models.
- THDR-NPs effectively inhibited tumor metastasis, indicating their potential for advanced cancer treatment.
Conclusions:
- The developed THDR-NPs showed superior efficacy compared to free dasatinib and rosiglitazone.
- This nanoparticle-based drug delivery system holds promise for treating breast cancer metastasis.
- The findings support the application of nanoparticles in organ-specific cancer therapies.
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