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Simvastatin-Loaded Polymeric Nanoparticles: Targeting Inflammatory Macrophages for Local Adipose Tissue Browning in Obesity Treatment
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    Simvastatin-Loaded Polymeric Nanoparticles: Targeting Inflammatory Macrophages for Local Adipose Tissue Browning in Obesity Treatment
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    • Neda Mohaghegh
      Neda Mohaghegh
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
    • Amir Ahari
      Amir Ahari
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      Department of Surgery, University of California-Los Angeles, Los Angeles, California 90095, United States
      More by Amir Ahari
    • Claire Buttles
      Claire Buttles
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      Department of Biology, Indiana University Bloomington, Bloomington, Indiana 47405, United States
    • Saya Davani
      Saya Davani
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      Department of Neurobiology, Physiology, and Behavior, University of California Davis, Briggs Hall, Davis, California 95616, United States
      More by Saya Davani
    • Hanna Hoang
      Hanna Hoang
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      Department of Microbiology, Immunology, and Molecular Genetics, University of California, Los Angeles, California 90024, United States
      More by Hanna Hoang
    • Qiang Huang
      Qiang Huang
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      More by Qiang Huang
    • Yixuan Huang
      Yixuan Huang
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      More by Yixuan Huang
    • Bahareh Hosseinpour
      Bahareh Hosseinpour
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      Department of Chemistry, Carleton University, Ottawa, Ontario K1S 5B6, Canada
    • Reza Abbasgholizadeh
      Reza Abbasgholizadeh
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
    • Andrea L. Cottingham
      Andrea L. Cottingham
      Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, Maryland 21201, United States
    • Neda Farhadi
      Neda Farhadi
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      More by Neda Farhadi
    • Mohsen Akbari
      Mohsen Akbari
      Department of Mechanical Engineering, University of Victoria, Victoria, British Columbia V8P 5C2, Canada
      Biotechnology Center, Silesian University of Technology, Gliwice 44-100, Poland
    • Heemin Kang
      Heemin Kang
      Department of Materials Science and Engineering, Korea University, Seoul 02841, Republic of Korea
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    • Ali Khademhosseini
      Ali Khademhosseini
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
    • Vadim Jucaud
      Vadim Jucaud
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      More by Vadim Jucaud
    • Ryan M. Pearson
      Ryan M. Pearson
      Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, Maryland 21201, United States
    • Alireza Hassani Najafabadi*
      Alireza Hassani Najafabadi
      Terasaki Institute for Biomedical Innovation, Los Angeles, California 90064, United States
      *E-mail: [email protected]
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    ACS Nano

    Cite this: ACS Nano 2024, 18, 40, 27764–27781
    Click to copy citationCitation copied!
    https://doi.org/10.1021/acsnano.4c10742
    Published September 29, 2024
    Copyright © 2024 American Chemical Society

    Abstract

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    Obesity is defined as chronic, low-grade inflammation within specific tissues. Given the escalating prevalence of obesity among individuals of all ages, obesity has reached epidemic proportions, posing an important public health challenge. Despite significant advancements in treating obesity, conventional approaches remain largely ineffective or involve severe side effects, thus underscoring the pressing need to explore and develop treatment approaches. Targeted and local immunomodulation using nanoparticles (NPs) can influence fat production and utilization processes. Statins, known for their anti-inflammatory properties, show the potential for mitigating obesity-related inflammation. A localized delivery option offers several advantages over oral and parenteral delivery methods. Here, we developed simvastatin (Sim) encapsulated within PLGA NPs (Sim-NP) for localized delivery of Sim to adipose tissues (ATs) for immunomodulation to treat obesity. In vitro experiments revealed the strong anti-inflammatory effects of Sim-NPs, which resulted in enhanced modulation of macrophage (MΦ) polarization and induction of AT browning. We then extended our investigation to an in vivo mouse model of high-fat-diet (HFD)-induced obesity. Sim-NP administration led to the controlled release of Sim within AT, directly impacting MΦ activity and inducing AT browning while inducing weight loss. Our findings demonstrated that Sim-NP administration effectively inhibited the progression of obesity-related inflammation, controlled white fat production, and enhanced AT modulation. These results highlight the potential of Sim-NP as a potent nanotherapy for treating obesity by modulating the immune system.

    Copyright © 2024 American Chemical Society

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    Supporting Information

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    The Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acsnano.4c10742.

    • Stability and structural integrity study revealing that Sim-NPs undergo controlled degradation, eventually releasing Sim, indicating their potential for sustained delivery under serum conditions (Figure S1); Sim-NPs did not exhibit cytotoxicity, as evidenced by the maintained metabolic activity and viability of BMDMs (Figure S2); Sim-NP enhances M2 macrophage differentiation in BMDMs, elevating anti-inflammatory macrophage levels (Figure S3); release profile of Sim from Sim-NP over 30 days (Figure S4) (PDF)

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    ACS Nano

    Cite this: ACS Nano 2024, 18, 40, 27764–27781
    Click to copy citationCitation copied!
    https://doi.org/10.1021/acsnano.4c10742
    Published September 29, 2024
    Copyright © 2024 American Chemical Society

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