We report here that the release mechanism of free camptothecin from self-assembling drug amphiphiles can be regulated by use of different linker groups. Our results highlight the significance of the linker group of drug amphiphiles on the drug release efficiency and their consequent in vitro efficacy.
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http://dx.doi.org/10.1039/c3cc49453e | DOI Listing |
Chemistry
January 2025
Indian Institute of Science Education and Research Thiruvananthapuram, Chemistry, Trivandrum, Trivandrum, Trivandrum, 695551, Trivandrum, INDIA.
Recent years have witnessed the rapid growth of combination therapy for the treatment of cancer. Chemo and antisense DNA therapies are two clinically proven and efficient treatment modalities for cancer. However, direct delivery of both chemo and antisense oligonucleotides into the cancerous cells is challenging and hence there is a high demand for the development of new strategies that permit the direct delivery of chemo and antisense therapeutic agents in a targeted fashion.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
NCNST: National Center for Nanoscience and Technology, CAS Key Lab for Biomedical Effects of Nanomaterials and Nanosafety, No 11, Zhongguancun Beiyitiao, Haidian, 100190, Beijing, CHINA.
Cisplatin (CP) is a first-line platinum-based drug used for the treatment of head and neck cancer. However, tumor cells can diminish the therapeutic effects of CP through the detoxification system mediated by glutathione (GSH) and the nucleotide excision repair (NER) pathway. Herein, we present a light-activable and pH-responsive oxidative stress nanoamplifier (FPLC@IR OSNA), comprising an amphiphilic compound (FPLC) with Fmoc-lysine acting as a connector between a nitroimidazole derivative and a pH-responsive cinnamaldehyde (CA) derivative, loaded with photosensitizer IR780.
View Article and Find Full Text PDFChemistry
January 2025
Kobe University, Department of Chemical Science & Engineering, 1-1 Rokkodaicho, Nada-ku, 657-8501, Kobe, JAPAN.
Organelle targeting is a useful approach in drug development for cancer therapy. Peptide amphiphiles are good candidates for targeting specific organelles because they can be engineered into a wide range of molecular structures, enabling customization for specific functional needs. We have developed a peptide amphiphile, C16-(EY)3, that can respond to tyrosine kinase activity and undergo phosphorylation inside cancer cells.
View Article and Find Full Text PDFNanoscale
January 2025
School of Applied and Interdisciplinary Sciences, Indian Association for the Cultivation of Science (IACS), 2A and 2B Raja. S. C. Mullick Road, Jadavpur, Kolkata 700032, India.
Water-soluble π-conjugated luminescent bioprobes have been broadly used in biomedical research but are limited by the nonbiodegradability associated with their rigid C-C backbones. In the present work, we introduced three naphthalene monoimide (NMI)-functionalized amphiphilic fluorescent polyesters (P1, P2, and P3) prepared by transesterification of functional diols with an activated diester monomer of adipic acid. These polyesters featured a side-chain NMI fluorophore, imparting the required hydrophobicity for self-assembly in water and endowing the polymeric nanoassemblies with green fluorescence.
View Article and Find Full Text PDFActa Biomater
January 2025
Hengyang Medical School, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, School of Pharmaceutical Science, MOE Key Lab of Rare Pediatric Disease, University of South China, Hengyang 421001, China. Electronic address:
Immune checkpoint blockers (ICBs)-based immunotherapy is a favorable approach for efficient triple-negative breast cancer (TNBC) treatment. However, the therapeutic efficacy of ICBs is greatly compromised by immunosuppressive tumor microenvironments (TMEs) and low expression levels of programmed cell death ligand-1 (PD-L1). Herein, we constructed an amphiphilic prodrug by linking a hydrophobic STING agonist, MSA-2 and a hydrophilic chemotherapeutic drug, gemcitabine (GEM) via an ester bond, which can self-assemble into GEM-MSA-2 (G-M) nanoparticles (NPs) with a tumor growth inhibition (TGI) value of 87.
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