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Dual Stimuli-Responsive Supramolecular Self-Assemblies Based on the Host-Guest Interaction between β-Cyclodextrin and
JianGuo Zhang1, Zi-Hao Zhou1, Lin Li1
1Key Laboratory of Macromolecular Science of Shaanxi Province, School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an 710062, P.R. China.
Abstract:
Health has always been a hot topic of concern, whereas cancer is one of the largest security risks to human health. Although the existing drug delivery systems (DDSs) have been extensively reported and commercially applied, there are still some issues that have yet to be well-resolved, including the toxicity, side-effects, and targeted therapy efficiency of drugs. Consequently, it is still necessary to develop a novel, highly efficient, controlled and targeted DDS for cancer therapy. For this, a supramolecular polymer, β-CD-g-PDMAEMA@Azo-PCL, was designed and developed through the host-guest inclusion complexation interactions between a host polymer, β-cyclodextrin-graft-poly(2-(dimethylamino)ethyl methacrylate) (β-CD-g-PDMAEMA), and a guest polymer, azobenzene modified poly(ε-caprolactone) (Azo-PCL), and was characterized by various analysis techniques. The supramolecular assembly was examined in various pH environments and/or under UV-vis irradiation, showing the formation of supramolecular assemblies from regular spherical shapes to irregular aggregates with various hydrodynamic diameters. The 2D NOESY NMR studies showed the formation of inclusion complexation between Azo-PCL and β-CD-g-PDMAEMA and between β-CD and the side groups of PDMAEMA. The supramolecular assemblies could encapsulate doxorubicin to form spherical core-shell drug-carrying micelles with an entrapment efficiency of 66.1%. The effects of external environment stimuli on the in vitro drug release were investigated, showing light- and pH-modulated drug release properties. The cytotoxicity assessment indicated that the blank supramolecular micelles were nontoxic, whereas the drug-loaded micelles exhibited comparable or even superior anticancer activity to the anticancer activity of free DOX and inhibition of cancer cell proliferation. Therefore, the developed supramolecular assemblies can potentially be used as drug-controlled release carriers.
Insights
A novel supramolecular polymer drug delivery system (DDS) was developed for targeted cancer therapy. This system effectively encapsulates chemotherapy drugs, enabling controlled release and enhanced anticancer activity with reduced toxicity.
Area of Science:
- Biomaterials Science
- Polymer Chemistry
- Nanotechnology
Background:
- Existing cancer drug delivery systems (DDSs) face challenges with drug toxicity, side effects, and targeted therapy efficiency.
- There is a continuous need for advanced DDSs that offer improved control, targeting, and efficacy in cancer treatment.
Purpose of the Study:
- To design and develop a novel supramolecular polymer, β-cyclodextrin-graft-poly(2-(dimethylamino)ethyl methacrylate)@azobenzene modified poly(ε-caprolactone) (β-CD-g-PDMAEMA@Azo-PCL), for targeted cancer therapy.
- To investigate the stimuli-responsive drug release capabilities and in vitro anticancer efficacy of the developed DDS.
Main Methods:
- Host-guest inclusion complexation between β-CD-g-PDMAEMA and Azo-PCL to form supramolecular assemblies.
- Characterization of supramolecular assembly formation under varying pH and UV-vis irradiation using techniques like NMR.
- Encapsulation of doxorubicin (DOX) into the supramolecular assemblies to form drug-loaded micelles.
- In vitro drug release studies under different environmental stimuli (pH, light).
- Cytotoxicity and anticancer activity assessments using cancer cell lines.
Main Results:
- The supramolecular polymer successfully formed assemblies with tunable structures in response to pH and UV-vis light.
- Host-guest complexation was confirmed via 2D NOESY NMR studies.
- Drug-loaded micelles achieved a high doxorubicin entrapment efficiency of 66.1%.
- The DDS demonstrated significant light- and pH-modulated in vitro drug release.
- Drug-loaded micelles showed potent anticancer activity comparable or superior to free doxorubicin, with minimal toxicity from blank micelles.
Conclusions:
- The developed β-CD-g-PDMAEMA@Azo-PCL supramolecular assemblies represent a promising platform for controlled and targeted cancer drug delivery.
- The stimuli-responsive nature of the DDS allows for precise control over drug release at the tumor site.
- This novel DDS holds potential for improving the efficacy and safety of cancer chemotherapy.
