ArticleBiomaterials2013
The effect of the acid-sensitivity of 4-(N)-stearoyl gemcitabine-loaded micelles on drug resistance caused by RRM1 overexpression.
Article in Biomaterials, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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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
28 citing papers in PubMed, 63 citations in OpenAlex.
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- Co-Delivery of Dacarbazine and miRNA 34a Combinations to Synergistically Improve Malignant Melanoma Treatments.Drug design, development and therapy · 2025Article
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- Effect of nanoparticle size on their distribution and retention in chronic inflammation sites.Discover nano · 2023Article
- Strategies to improve the physicochemical properties of peptide-based drugs.Pharmaceutical research · 2023Review
- Emerging pro-drug and nano-drug strategies for gemcitabine-based cancer therapy.Asian journal of pharmaceutical sciences · 2022Review
- Lipid-Based Drug Delivery Systems in Regenerative Medicine.Materials (Basel, Switzerland) · 2021Review
- Effect of surface mannosylation on the cytotoxicity and cellular uptake of stearoyl gemcitabine-incorporated, acid-sensitive micelles.Colloid and interface science communications · 2021Article
- PD-1 siRNA-Encapsulated Solid Lipid Nanoparticles Downregulate PD-1 Expression by Macrophages and Inhibit Tumor Growth : PD-1 siRNA-Encapsulated Solid Lipid Nanoparticles.AAPS PharmSciTech · 2021Article
- Light-Responsive Micelles Loaded With Doxorubicin for Osteosarcoma Suppression.Frontiers in pharmacology · 2021Article
- Applications of RNA interference in the treatment of arthritis.Translational research : the journal of laboratory and clinical medicine · 2019Review
- Ectopic high endothelial venules in pancreatic ductal adenocarcinoma: A unique site for targeted delivery.EBioMedicine · 2018Article
- Lipid nanoparticles with minimum burst release of TNF-α siRNA show strong activity against rheumatoid arthritis unresponsive to methotrexate.Journal of controlled release : official journal of the Controlled Release Society · 2018Article
- Overcoming tumor cell chemoresistance using nanoparticles: lysosomes are beneficial for (stearoyl) gemcitabine-incorporated solid lipid nanoparticles.International journal of nanomedicine · 2018Review
- Pancreatic Cancer Chemoresistance to Gemcitabine.Cancers · 2017Review
- Phase-Separated Liposomes Enhance the Efficiency of Macromolecular Delivery to the Cellular Cytoplasm.Cellular and molecular bioengineering · 2017Article
- Lipid-Drug Conjugate for Enhancing Drug Delivery.Molecular pharmaceutics · 2017Review
- Acid-Sensitive Sheddable PEGylated PLGA Nanoparticles Increase the Delivery of TNF-α siRNA in Chronic Inflammation Sites.Molecular therapy. Nucleic acids · 2016Article
- Tumor-Associated Macrophage-Mediated Targeted Therapy of Triple-Negative Breast Cancer.Molecular pharmaceutics · 2016Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Chemoresistance is a major issue for most gemcitabine-related chemotherapies. The overexpression of ribonucleotide reductase subunit M1 (RRM1) plays a key role in gemcitabine resistance. In this study, we synthesized a new highly acid-sensitive amphiphilic micelle material by conjugating hydrophilic polyethylene glycol with a hydrophobic stearic acid derivative (C18) using a hydrazone bond, which was named as PHC-2. A lipophilic prodrug of gemcitabine, 4-(N)-stearoyl gemcitabine (GemC18), was loaded into micelles prepared with PHC-2, a previously synthesized less acid-sensitive PHC-1, and their acid-insensitive counterpart, PAC. GemC18 loaded in acid-sensitive micelles can overcome gemcitabine resistance, and GemC18 in the highly acid-sensitive PHC-2 micelles was more cytotoxic than in the less acid-sensitive PHC-1 micelles. Mechanistic studies revealed that upon cellular uptake and lysosomal delivery, GemC18 in the acid-sensitive micelles was released and hydrolyzed more efficiently. Furthermore, GemC18 loaded in the highly acid-sensitive PHC-2 micelles inhibited the expression of RRM1 and increased the level of gemcitabine triphosphate (dFdCTP) in gemcitabine resistant tumor cells. The strategy of delivering lipophilized nucleoside analogs using highly acid-sensitive micelles may represent a new platform technology to increase the antitumor activity of nucleoside analogs and to overcome tumor cell resistance to them.
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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.