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Updated: Mar 6, 2026
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Soluplus/TPGS mixed micelles for dioscin delivery in cancer therapy
Jing Zhao1, Youwei Xu1, Changyuan Wang1
1a School of Pharmacy, Dalian Medical University , Dalian , P.R. China.
Background:
Dioscin has shown cytotoxicity against cancer cells, but its poor solubility and stability have limited its clinical application. In this study, we designed mixed micelles composed of TPGS and Soluplus® copolymers entrapping the poorly soluble anticancer drug dioscin.
Method:
In order to improve the aqueous solubility and bioactivity of dioscin, TPGS/Soluplus® mixed micelles with an optimal ratio were prepared using a thin-film hydration method, and their physicochemical properties were characterized. Cellular cytotoxicity and uptake of the dioscin-loaded TPGS/Soluplus® mixed micelles were studied in MCF-7 breast cancer cells and A2780s ovarian cancer cells. The pharmacokinetics of free dioscin and dioscin-loaded TPGS/Soluplus® mixed micelles was studied in vivo in male Sprague-Dawley rats via a single intravenous injection in the tail vein.
Results:
The average size of the optimized mixed micelle was 67.15 nm, with 92.59% drug encapsulation efficiency and 4.63% drug loading efficiency. The in vitro release profile showed that the mixed micelles presented sustained release behavior compared to the anhydrous ethanol solution of dioscin. In vitro cytotoxicity assays were conducted on human cancer cell lines including A2780s ovarian cancer cells and MCF-7 breast cancer cells. The mixed micelles exhibited better antitumor activity compared to free dioscin against all cell lines, which may benefit from the significant increase in the cellular uptake of dioscin from mixed micelles compared to free dioscin. The pharmacokinetic study showed that the mixed micelle formulation achieved a 1.3 times longer mean residual time (MRT) in circulation and a 2.16 times larger area under the plasma concentration-time curve (AUC) than the free dioscin solution.
Conclusion:
Our results suggest that the dioscin-loaded mixed micelles developed in this study might be a potential nano drug-delivery system for cancer chemotherapy.
Insights
This study developed mixed micelles to improve the anticancer drug dioscin
Area of Science:
- Nanotechnology
- Materials Science
- Pharmacology
Background:
- Dioscin exhibits anticancer properties but faces limitations due to poor solubility and stability.
- Traditional drug delivery hinders dioscin's clinical efficacy.
- Novel formulations are needed to enhance dioscin's therapeutic potential.
Purpose of the Study:
- To develop a nano drug-delivery system for dioscin using TPGS/Soluplus® mixed micelles.
- To improve dioscin's aqueous solubility, stability, and anticancer activity.
- To evaluate the physicochemical properties, in vitro cytotoxicity, and in vivo pharmacokinetics of the novel formulation.
Main Methods:
- TPGS/Soluplus® mixed micelles encapsulating dioscin were prepared via thin-film hydration.
- Physicochemical properties, including size and drug loading, were characterized.
- In vitro cytotoxicity and cellular uptake were assessed in MCF-7 and A2780s cancer cell lines.
- In vivo pharmacokinetic studies were conducted in Sprague-Dawley rats.
Main Results:
- Optimized mixed micelles demonstrated high encapsulation efficiency (92.59%) and sustained drug release.
- Dioscin-loaded mixed micelles showed enhanced cytotoxicity against breast and ovarian cancer cells compared to free dioscin.
- In vivo studies revealed improved pharmacokinetic profiles, with a longer mean residual time and larger AUC for the micelle formulation.
- Increased cellular uptake of dioscin was observed from the mixed micelles.
Conclusions:
- TPGS/Soluplus® mixed micelles represent a promising nano drug-delivery system for dioscin.
- This formulation enhances dioscin's solubility, stability, and anticancer efficacy.
- The developed system holds potential for improving cancer chemotherapy outcomes.
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