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Updated: May 10, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
A β-cyclodextrin-based supramolecular modular system creating micellar carriers for codelivery of doxorubicin and
Xichuan Tang1, Yuting Wen2, Zhongxing Zhang1
1Department of Biomedical Engineering, College of Design and Engineering, National University of Singapore, 15 Kent Ridge Crescent, Singapore 119276, Singapore.
Abstract:
The combination of chemotherapy and gene therapy holds promise in treating cancer. A key strategy is to use small interfering RNAs (siRNAs) to silence programmed death-ligand 1 (PD-L1) expression in cancer cells, disrupting tumor immune evasion and enhancing anticancer treatments, particularly when used in conjunction with chemotherapy drugs such as doxorubicin (Dox). However, effective codelivery of drugs and genes requires carefully designed carriers and complex synthesis procedures. To address this challenge, we propose a convenient modular self-assembly system for creating multifunctional micellar carriers that can efficiently codeliver both Dox and siRNA, where micelles are formed by cationic amphiphilic supramolecular architectures that are constructed through host-guest interactions between β-cyclodextrin (β-CD) and adamantane (Ad) to incorporate various functional polymer segments, such as low-molecular-weight polyethylenimine (oligoethylenimine, OEI), poly(ethylene glycol) (PEG), and polycaprolactone (PCL), at adjustable ratios. The supramolecular micellar carrier systems can be easily optimized to achieve excellent structural stability, drug and gene loading, and delivery efficiency, resulting in significant anticancer effects from Dox delivery and simultaneous inhibition of PD-L1 due to the siRNA delivery. Therefore, this modular supramolecular strategy offers a sophisticated, adaptable, and straightforward approach to creating multifunctional micellar carriers, with potential for drug- and gene-based immune-assisted cancer therapy.
Insights
This study introduces a modular self-assembly system for creating micellar carriers that efficiently codeliver chemotherapy drugs and small interfering RNAs (siRNAs) to target cancer cells and inhibit PD-L1 expression, enhancing cancer therapy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Therapy
Background:
- Chemotherapy and gene therapy combination shows promise for cancer treatment.
- Silencing PD-L1 with small interfering RNAs (siRNAs) can enhance anticancer immunity.
- Effective codelivery of drugs and genes is challenging due to carrier design and synthesis complexity.
Purpose of the Study:
- To develop a convenient modular self-assembly system for multifunctional micellar carriers.
- To achieve efficient codelivery of doxorubicin (Dox) and siRNA for cancer treatment.
- To create adaptable carriers for drug- and gene-based immune-assisted cancer therapy.
Main Methods:
- Utilized host-guest interactions between β-cyclodextrin (β-CD) and adamantane (Ad) for micelle formation.
- Incorporated functional polymer segments like oligoethylenimine (OEI), poly(ethylene glycol) (PEG), and polycaprolactone (PCL) at adjustable ratios.
- Engineered cationic amphiphilic supramolecular architectures for drug and gene encapsulation.
Main Results:
- Demonstrated efficient codelivery of Dox and siRNA using the developed micellar carriers.
- Achieved excellent structural stability, drug and gene loading, and delivery efficiency.
- Observed significant anticancer effects from Dox delivery and PD-L1 inhibition via siRNA.
Conclusions:
- The modular supramolecular strategy provides a straightforward approach to create multifunctional micellar carriers.
- This system enables adaptable and efficient codelivery of drugs and genes for cancer therapy.
- The developed carriers hold potential for advancing drug- and gene-based immune-assisted cancer treatment.
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Site-Targeted Drug Delivery Systems: Polymeric Carriers

