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Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
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Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...

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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
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[Anticancer effect of triptolide-polyethylenimine-cyclodextrin in vitro].

Tian-nan Hu1, Qi-wen Wang, Xue Jin

  • 1Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou, China.

Zhejiang Da Xue Xue Bao. Yi Xue Ban = Journal of Zhejiang University. Medical Sciences
|December 15, 2012
PubMed
Summary

This study developed a novel triptolide-polyethylenimine-cyclodextrin drug delivery system. The system effectively inhibits cancer cell growth and delivers siRNA, showing potential for combined gene and drug cancer therapy.

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Cancer Therapeutics

Context:

  • Developing novel drug delivery systems is crucial for effective cancer treatment.
  • Targeted delivery of both therapeutic agents and genetic material can enhance efficacy.
  • Triptolide is a potent anticancer compound with limitations in delivery.

Purpose:

  • To synthesize and characterize a triptolide-polyethylenimine-cyclodextrin conjugate.
  • To evaluate the in vitro anticancer activity of the developed system.
  • To assess the system's capability for co-delivery of siRNA and triptolide.

Summary:

  • Triptolide was successfully conjugated to polyethylenimine-cyclodextrin, confirmed by NMR, FT-IR, and XRD.
  • The resulting triptolide-polyethylenimine-cyclodextrin system demonstrated significant in vitro anticancer effects and low cytotoxicity.
  • The system effectively condensed siRNA (particle size 300±15 nm, zeta potential 8±2.5 mV) and delivered it into cancer cell cytoplasm.

Impact:

  • The triptolide-polyethylenimine-cyclodextrin system inhibits cancer cell growth and migration in vitro.
  • This novel system shows promise as a prodrug for the co-delivery of genes and drugs in cancer therapy.
  • Facilitates advanced therapeutic strategies through combined gene and drug delivery.