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Updated: Jul 31, 2025
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Anticancer Evaluation of Methoxy Poly(Ethylene Glycol)-b-Poly(Caprolactone) Polymeric Micelles Encapsulating
Yu Been Shin1, Ju-Yeon Choi2, Dae Hwan Shin1
1College of Pharmacy, Chungbuk National University, Cheongju, 28160, Republic of Korea.
Purpose:
We aimed to inhibit ovarian cancer (OC) development by interfering with microtubule polymerization and inhibiting mTOR signaling. To achieve this, previously developed micelles containing fenbendazole and rapamycin were applied.
Methods:
Herein, we prepared micelles for drug delivery using fenbendazole and rapamycin at a 1:2 molar ratio and methoxy poly(ethylene glycol)-b-poly(caprolactone)(mPEG-b-PCL) via freeze-drying. We revealed their long-term storage capacity of up to 120 days. Furthermore, a cytotoxicity test was performed on the OC cell line HeyA8, and an orthotopic model was established for evaluating in vivo antitumor efficacy.
Results:
Fenbendazole/rapamycin-loaded mPEG-b-PCL micelle (M-FR) had an average particle size of 37.2 ± 1.10 nm, a zeta potential of -0.07 ± 0.09 mV, and a polydispersity index of 0.20 ± 0.02. Additionally, the average encapsulation efficiency of fenbendazole was 75.7 ± 4.61% and that of rapamycin was 98.0 ± 1.97%. In the clonogenic assay, M-FR was 6.9 times more effective than that free fenbendazole/rapamycin. The in vitro drug release profile showed slower release in the combination formulation than in the single formulation.
Conclusion:
There was no toxicity, and tumor growth was suppressed substantially by our formulation compared with that seen with the control. The findings of our study lay a foundation for using fenbendazole and rapamycin for OC treatment.
Insights
This study developed stable micelles loaded with fenbendazole and rapamycin to treat ovarian cancer (OC). The formulation significantly suppressed tumor growth with no observed toxicity, paving the way for novel OC therapies.
Area of Science:
- Nanomedicine
- Cancer Biology
- Pharmacology
Background:
- Ovarian cancer (OC) remains a significant health challenge, necessitating novel therapeutic strategies.
- Targeting microtubule polymerization and mTOR signaling pathways are promising avenues for OC treatment.
- Developing effective drug delivery systems is crucial for enhancing therapeutic efficacy and reducing side effects.
Purpose of the Study:
- To inhibit ovarian cancer (OC) development by interfering with microtubule polymerization and mTOR signaling.
- To formulate and characterize stable micelles encapsulating fenbendazole and rapamycin for OC treatment.
- To evaluate the in vitro and in vivo efficacy of the developed micellar formulation.
Main Methods:
- Micelles were prepared using fenbendazole, rapamycin, and mPEG-b-PCL via freeze-drying.
- Micelles (M-FR) were characterized for particle size, zeta potential, and encapsulation efficiency.
- Cytotoxicity was assessed using the OC cell line HeyA8, and in vivo antitumor efficacy was evaluated in an orthotopic OC model.
Main Results:
- Fenbendazole/rapamycin-loaded mPEG-b-PCL micelles (M-FR) exhibited favorable physicochemical properties (37.2 nm size, PDI 0.20).
- M-FR demonstrated superior efficacy (6.9 times) in clonogenic assays compared to free drugs.
- In vitro release studies showed sustained drug release from the combination formulation, and in vivo studies confirmed substantial tumor growth suppression without toxicity.
Conclusions:
- The developed fenbendazole/rapamycin-loaded micelles are stable and demonstrate enhanced efficacy for ovarian cancer treatment.
- The formulation effectively inhibits tumor growth in vivo with no observed toxicity.
- These findings provide a strong foundation for the clinical application of fenbendazole and rapamycin in ovarian cancer therapy.
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