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Updated: May 28, 2025
Synthesis of Stimuli-responsive Nanogels using Aqueous One-step Crosslinking and Co-nanopolymerization
Published on: January 24, 2025
Natural polysaccharide-small molecule smart responsive nanogels: Design, synthesis, and synergistic
Sibei Wang1, Fan Nie1, Zhen Lin1
1State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, People's Republic of China.
Abstract:
Cancer poses a significant medical challenge worldwide. Research into tumor biology has revealed the prevalence of acidic conditions and abnormally high levels of reactive oxygen species (ROS) within the tumor microenvironment. In response to these findings, a ROS-responsive crosslinker, (((oxalylbis(oxy))bis(methylene))bis(4,1-phenylene))diboronic acid (OBA), was designed and synthesized using (4-hydroxymethyl)phenylboronic acid and ethanedioyl chloride as reactants. pH-responsive boronate ester bonds were formed between the diboronic acid groups of the crosslinker and the dihydroxyl groups of the naturally occurring active Astragalus polysaccharide (ASP). This resulted in the successful construction of pH/ROS dual-responsive nanogels (BAI@ASPOBA) loaded with the chemotherapeutic natural small molecule baicalein (BAI). Characterization of BAI@ASPOBA through molecular dynamics simulations and other methods demonstrated that it not only inhibited the proliferation of A549 tumor cells in vitro but also exhibited remarkable anti-tumor activity in vivo, along with excellent safety and biocompatibility. Further mechanistic studies revealed that the anti-tumor activity arises from the synergistic enhancement of the chemotherapeutic effects of BAI and the natural polysaccharide ASP. Specifically, the constructed BAI@ASPOBA nanogels enhanced the anti-tumor efficacy of BAI, while ASP, serving as the carrier for the nanomaterials, played an immunostimulatory role, facilitating tumor immunotherapy. The design and development of the novel BAI@ASPOBA nanogels in this study are anticipated to provide a new and effective treatment strategy for cancer therapy.
Insights
New nanogels combat cancer by targeting acidic tumor environments and reactive oxygen species (ROS). These dual-responsive nanogels loaded with baicalein (BAI) show potent anti-tumor effects and enhance immunotherapy.
Area of Science:
- Biomaterials Science
- Cancer Research
- Nanotechnology
Background:
- The tumor microenvironment is characterized by acidity and high reactive oxygen species (ROS) levels, presenting therapeutic challenges.
- Developing targeted drug delivery systems is crucial for effective cancer treatment.
- Natural polysaccharides offer potential as biocompatible carriers for chemotherapeutics.
Purpose of the Study:
- To design and synthesize novel pH/ROS dual-responsive nanogels for cancer therapy.
- To load the chemotherapeutic agent baicalein (BAI) into these nanogels.
- To evaluate the in vitro and in vivo anti-tumor efficacy and biocompatibility of the developed nanogels.
Main Methods:
- Synthesis of a ROS-responsive crosslinker, (((oxalylbis(oxy))bis(methylene))bis(4,1-phenylene))diboronic acid (OBA).
- Formation of pH-responsive boronate ester bonds between OBA and Astragalus polysaccharide (ASP).
- Construction and characterization of baicalein-loaded dual-responsive nanogels (BAI@ASPOBA) using molecular dynamics simulations and in vitro/in vivo assays.
Main Results:
- Successful construction of pH/ROS dual-responsive nanogels (BAI@ASPOBA) loaded with baicalein.
- BAI@ASPOBA demonstrated significant inhibition of A549 tumor cell proliferation in vitro.
- In vivo studies showed remarkable anti-tumor activity, excellent safety, and biocompatibility of BAI@ASPOBA.
- Mechanistic studies revealed synergistic anti-tumor effects from BAI's chemotherapy and ASP's immunostimulatory role.
Conclusions:
- The novel BAI@ASPOBA nanogels represent a promising strategy for cancer therapy by leveraging dual-responsiveness to the tumor microenvironment.
- The nanogels enhance the efficacy of baicalein chemotherapy and facilitate tumor immunotherapy through the Astragalus polysaccharide carrier.
- This approach offers a new and effective treatment modality for cancer, combining targeted drug delivery with immunomodulation.
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