ArticlePharmaceutical research2012
Formulation and characterization of polyester/polycarbonate nanoparticles for delivery of a novel microtubule destabilizing agent.
Article in Pharmaceutical research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- A Pyrimidine-Based Tubulin Inhibitor Shows Potent Anti-Glioblastoma Activity In Vitro and In Vivo.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Fused Imidazopyrazine-Based Tubulin Polymerization Inhibitors Inhibit Neuroblastoma Cell Function.ACS medicinal chemistry letters · 2023Article
- Design, Synthesis, and Biological Evaluation of Pyrimidine Dihydroquinoxalinone Derivatives as Tubulin Colchicine Site-Binding Agents That Displayed Potent Anticancer Activity Both In Vitro and In Vivo.ACS pharmacology & translational science · 2023Article
- X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.Journal of medicinal chemistry · 2021Article
- Nanoformulation design and therapeutic potential of a novel tubulin inhibitor in pancreatic cancer.Journal of controlled release : official journal of the Controlled Release Society · 2021Article
- Nanoparticulate delivery of potent microtubule inhibitor for metastatic melanoma treatment.Journal of controlled release : official journal of the Controlled Release Society · 2019Article
- Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy.Journal of medicinal chemistry · 2018Article
- Design, Synthesis and Biological Evaluation of novel Hedgehog Inhibitors for treating Pancreatic Cancer.Scientific reports · 2017Article
- Current Advances of Tubulin Inhibitors in Nanoparticle Drug Delivery and Vascular Disruption/Angiogenesis.Molecules (Basel, Switzerland) · 2016Review
- Systemic delivery of nanoparticle formulation of novel tubulin inhibitor for treating metastatic melanoma.Drug delivery and translational research · 2015Article
- Nanoparticle-mediated drug delivery for treating melanoma.Nanomedicine (London, England) · 2015Review
- LHRH-conjugated micelles for targeted delivery of antiandrogen to treat advanced prostate cancer.Pharmaceutical research · 2014Article
- Nanomedicines of Hedgehog inhibitor and PPAR-γ agonist for treating liver fibrosis.Pharmaceutical research · 2014Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
purposeSince our newly synthesized potent 5-indolyl derivative, (2-(1 H-Indol-5-yl) thiazol-4-yl) 3, 4, 5-trimethoxyphenyl methanone (LY293), to treat resistant melanoma was hydrophobic, our objective was to synthesize a biodegradable copolymer for formulating this drug into nanoparticles and to determine its anticancer activity and mechanism of action.
methodsMethoxy poly (ethylene glycol)-b-poly (carbonate-co-lactide) [mPEG-b-P (CB-co-LA)] was synthesized for formulating LY293 into nanoparticles by o/w emulsification and stabilization by solvent evaporation. Particle size, drug release profile, in vitro efficacy in multiple melanoma cells, and mechanism of action of drug-loaded nanoparticles were determined.
resultsLY293-loaded nanoparticles with 170 nm mean size and 2.2 and 4.16% drug loading efficiently inhibited proliferation of A375 and B16F10 cells with IC(50) of 12.5 nM and 25 nM, respectively. LY293 circumvented multidrug resistance and inhibited proliferation of Pgp overexpressing MDA-MB435/LCC6 MDR1 melanoma cells. Upon treatment with LY293-loaded nanoparticles, A375 cells underwent cell cycle arrest in G2/M phase and apoptotic cell death. Immunofluorescence images showed inhibition of tubulin polymerization after treatment with LY293.
conclusionLY293-loaded mPEG-b-P (CB-co-LA) nanoparticles showed excellent efficacy and induced apoptosis in melanoma cells. These polyester/polycarbonate-based nanoparticles provided an excellent platform to deliver different poorly soluble drugs to melanoma.
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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.