A novel water soluble and biodegradable cyclotriphosphazene-paclitaxel conjugate was prepared by reacting 2'-succinyl paclitaxel with cyclotriphosphazenes bearing equimolar glycyl-L-lysine and methoxy poly(ethylene glycol) as side groups. The macromolecular conjugate was found to self-assemble in aqueous solution to form stable micelles with a mean hydrodynamic diameter of 24.7 nm and a low critical micelle concentration of 10 mg/L. The present conjugate exhibited lower than free paclitaxel but reasonably high in vitro cytotoxicity against selected human tumor cells due to their hydrolytic degradation in PBS solution.
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http://dx.doi.org/10.1016/j.bmcl.2008.10.077 | DOI Listing |
J Med Chem
January 2025
Institute for Drug Research, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem 9112102, Israel.
Cisplatin and oxaliplatin are Pt(II) anticancer agents that are used to treat several cancers, usually in combination with other drugs. Their efficacy is diminished by dose-limiting peripheral neuropathy (PN) that affects ∼70% of patients. PN is caused by selective accumulation of the platinum drugs in the dorsal root ganglia (DRG), which overexpress transporters for cisplatin and oxaliplatin.
View Article and Find Full Text PDFJ Control Release
December 2024
Department of Urology, South China Hospital, Medical School, Shenzhen University, Shenzhen 518116, China; Institute of Urology, The Affiliated Luohu Hospital of Shenzhen University, Shenzhen University, Shenzhen 518000, China. Electronic address:
Cisplatin-based neoadjuvant chemotherapy is first-line strategy to inhibit progression and metastasis of muscle-invasive bladder cancer (MIBC). However, its clinical efficacy is often limited by drug resistance and severe systemic side effects, highlighting the urgent need for innovative therapeutic approaches. Despite advancements in cisplatin-based regimens, research on intravesical cisplatin delivery systems remains scarce.
View Article and Find Full Text PDFACS Macro Lett
January 2025
Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur, West Bengal 721302, India.
Despite having several advantages, bicontinuously structured polymeric nanoparticles (BSPNPs) are far less explored in the field of controlled drug delivery owing to the requirement of complex precursor copolymers and the associated multistep synthetic procedures. In this work, we report the synthesis of a redox-sensitive diblock copolymer (P1), which was subsequently utilized to prepare doxorubicin (DOX) containing a pH-labile prodrug (P2). P1 and P2 spontaneously self-assembled in aqueous media above their critical aggregation concentration, forming micellar nanoparticles with rare bicontinuous morphology that promotes loading of both hydrophobic and hydrophilic cargoes in different compartments.
View Article and Find Full Text PDFBiomacromolecules
January 2025
Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska 68198, United States.
Amphiphilic self-indicating and responsive polymer-based prodrugs have generated much interest as potential stimuli-responsive intelligent drug delivery systems (DDS) due to their ability to selectively deliver drugs to the cancer cells and to monitor real-time cellular uptake of the drug by imaging technique(s). In this direction, we have synthesized a new pH-responsive -vinyl-2-pyrrolidone and coumarin-based fluorescent self-indicating polymeric prodrug (SIPD), poly(NVP)--poly(FPA.DOX--FPA--CA).
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