ArticleJournal of controlled release : official journal of the Controlled Release Society2019
Formulation and preclinical evaluation of a toll-like receptor 7/8 agonist as an anti-tumoral immunomodulator.
Article in Journal of controlled release : official journal of the Controlled Release Society, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
43 citing papers in PubMed, 84 citations in OpenAlex.
- Prolonged intratumoral treatment with TLR7/8 agonist R848 regulates the tumor immune microenvironment resulting in enhanced antitumor activity.Cancer biology & therapy · 2026Article
- Dual Drug-Loaded Enzyme-Responsive Liposomes Exert Specific Modulation on Liver Cancer Cells and Tumor-Associated Macrophages In Vitro.Pharmaceutics · 2026Article
- Temporal Immune and Metabolic Shifts Drive the Anti-Tumor Efficacy of Resiquimod-Loaded Nanoparticles in Peritoneal Carcinomatosis.Advanced healthcare materials · 2026Article
- Tumor Microenvironmental Regulation of CAR T-Cell Therapy in High Risk Medulloblastoma.Research square · 2026Article
- Precise delivery and controlled release: strategies and advances in TLR7/8 agonist prodrugs for cancer immunotherapy.Frontiers in immunology · 2026Review
- A Systematic Review of Advanced Drug Delivery Systems: Engineering Strategies, Barrier Penetration, and Clinical Progress (2016-April 2025).Pharmaceutics · 2025Review
- X-ray-driven nanomotor with enhanced penetration and retention for carbon monoxide-amplified radioimmunotherapy of advanced colorectal cancer.Materials today. Bio · 2025Article
- Targeting pattern recognition receptors for cancer therapy: Mechanisms and strategies.Acta pharmaceutica Sinica. B · 2025Review
- Near-Infrared-Triggered Nanodroplets for Imaging-Guided Macrophage-Mediated Cancer Immunotherapy.Small methods · 2025Article
- Post-resection delivery of a TLR7/8 agonist from a biodegradable scaffold achieves immune-mediated glioblastoma clearance and protection against tumor challenge in mice.Nature communications · 2025Article
- Emerging therapeutics targeting tumor-associated macrophages for the treatment of solid organ cancers.Expert opinion on emerging drugs · 2025Review
- Self-assembly of paclitaxel derivative and fructose as a potent inducer of immunogenic cell death to enhance cancer immunotherapy.Materials today. Bio · 2025Article
- Nano-adjuvant based on lipo-imiquimod self-assembly for enhanced foot-and-mouth disease virus vaccine immune responsesMaterials today. Bio · 2025Article
- mRNA-LNP vaccine strategies: Effects of adjuvants on non-parenchymal liver cells and tolerance.Molecular therapy. Methods & clinical development · 2025Article
- Design, Synthesis, and Biological Evaluation of BODIPY-Caged Resiquimod as a Dual-Acting Phototherapeutic.Journal of medicinal chemistry · 2025Article
- Preliminary evaluation of the safety and feasibility of toll-like receptor ligand CB101 combined with hypofractionated radiation therapy in canine head and neck cancer: a pilot study.Veterinary oncology (London, England) · 2025Article
- All-Natural Gelatin-Based Nanoemulsion Loaded with TLR 7/8 Agonist for Efficient Modulation of Macrophage Polarization for Immunotherapy.Nanomaterials (Basel, Switzerland) · 2024Article
- Immunomodulatory R848-Loaded Anti-PD-L1-Conjugated Reduced Graphene Oxide Quantum Dots for Photothermal Immunotherapy of Glioblastoma.Pharmaceutics · 2024Article
- The tRNAProceedings of the National Academy of Sciences of the United States of America · 2024Article
- Revolutionizing head and neck squamous cell carcinoma treatment with nanomedicine in the era of immunotherapy.Frontiers in immunology · 2024Review
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
The toll-like receptor 7 and 8 (TLR7/8) agonist Resiquimod (R848) has been recognized as a promising immunostimulator for the treatment of cutaneous cancers in multiple clinical trials. However, systemic administration of R848 often results in strong immune-related toxicities while having limited therapeutic effects to the tumor. In the present study, a prodrug-based nanocarrier delivery system was developed that exhibited high therapeutic efficiency. R848 was conjugated to α-tocopherol to constitute an R848-Toco prodrug, followed by formulating with a tocopherol-modified hyaluronic acid (HA-Toco) as a polymeric nano-suspension. In vitro evaluation showed that the delivery system prolonged the release kinetics while maintaining TLR agonist activities. When administered subcutaneously, the nano-suspension formed a depot at the injection site, inducing localized immune responses without systemic expansion. This formulation also suppressed tumor growth and recruited immune cells to the tumor in a murine model of head and neck cancer. In a preclinical canine study of spontaneous mast cell tumors, the treatment led to a 67% response rate (three partial remissions and one complete remission).
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.