Aim: Glioblastoma multiforme is a devastating disease with no curative options due to the difficulty in achieving sufficient quantities of effective chemotherapies into the tumor past the blood-brain barrier. Micelles loaded with temozolomide (TMZ) were designed to increase the delivery of this drug into the brain.
Materials & Methods: pH-responsive micelles composed of distearoyl phosphoethanolamine-PEG-2000-amine and N-palmitoyl homocysteine were surface-functionalized with PDGF peptide and Dylight 680 fluorophore.
Results & Conclusion: PDGF-micelles containing TMZ have specific uptake and increased killing in glial cells compared with untargeted micelles. In vivo studies demonstrated selective accumulation of PDGF-micelles containing TMZ in orthotopic gliomas implanted in mice. Targeted micelle-based drug carrier systems hold potential for delivery of a wide variety of hydrophobic drugs thereby reducing its systemic toxicity.
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http://dx.doi.org/10.2217/nnm.15.218 | DOI Listing |
Int J Biol Macromol
January 2025
Iranian Research Organization for Science and Technology (IROST), Sh. Ehsani Rad St., Enqelab St., Ahmadabad Mostoufi Rd., Azadegan Highway, P. O. Box 33535-111, Tehran 3313193685, Iran.
Bacterial cellulose, with mechanical strength, high water absorption, and crystallinity, is used in eco-friendly packaging, wound dressings, and drug delivery systems. Despite its potential, industrial-scale production is limited by inefficiency and high costs, requiring high-yield strains and optimized growth conditions. This study found that indigenous isolates produce superior bacterial cellulose compared to standard strains.
View Article and Find Full Text PDFEur J Med Chem
January 2025
China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin, 300457, China. Electronic address:
A series of isatin derivatives which could inhibit colorectal cancer (CRC) were synthesized. Among those compounds, 5B exhibited good inhibitory activity of CRC through the inhibition of tubulin expression, inducing apoptosis, and causing G2/M phase cell cycle arrest pathway, which suggested that 5B could be a potential tubulin inhibitor. Based on that, a novel peptide-drug conjugate (PDC), which employed the CRC cells related receptor CD44 ligand peptide A6 coupling to 5B to accomplish A6-5B.
View Article and Find Full Text PDFBioorg Chem
January 2025
Department of Chemistry, Sarojini Naidu College for Women, Kolkata 700028, India. Electronic address:
Peptide nucleic acids (PNA), synthetic molecules comprising a peptide-like backbone and natural and unnatural nucleobases, have garnered significant attention for their potential applications in gene editing and other biomedical fields. The unique properties of PNA, particularly enhanced stability/specificity/affinity towards targeted DNA and RNA sequences, achieved significant attention recently for gene silencing, gene correction, antisense therapy, drug delivery, biosensing and other various diagnostic aspects. This review explores the structure, properties, and potential of PNA in transforming genetic engineering including potent biomedical challenges.
View Article and Find Full Text PDFACS Nano
January 2025
State Key Laboratory of Oral Diseases, National Center for Stomatology, National Clinical Research Center for Oral Diseases, West China Hospital of Stomatology, Sichuan University, Chengdu, Sichuan 610041, China.
Targeted drug delivery is a promising strategy for treating inflammatory diseases, with recent research focusing on the combination of neutrophils and nanomaterials. In this study, a targeted nanodrug delivery platform (Ac-PGP-tFNA, APT) was developed using tetrahedral framework nucleic acid (tFNA) along with a neutrophil hitchhiking mechanism to achieve precise delivery and anti-inflammatory effects. The tFNA structure, known for its excellent drug-loading capacity and cellular uptake efficiency, was used to carry a therapeutic agent─baicalin.
View Article and Find Full Text PDFJ Med Chem
January 2025
School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, PR China.
Sepsis is a systemic inflammatory response caused by infection and is a leading cause of death worldwide. We designed and synthesized a series of hederagenin analogues with anti-inflammatory activity. The most effective compound, , reduced the release of TNF-α and IL-6 in RAW264.
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