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Novel Fluorescent Benzimidazole-Hydrazone-Loaded Micellar Carriers for Controlled Release: Impact on Cell Toxicity,

Rayna Bryaskova1, Nikolai Georgiev2, Nikoleta Philipova1

  • 1Department of Polymer Engineering, University of Chemical Technology and Metallurgy, 8 Kliment Ohridsky Str., 1756 Sofia, Bulgaria.

Pharmaceutics
|June 28, 2023
PubMed

Insights

Novel fluorescent nanomicelles carrying an anticancer drug (BzH) were created for simultaneous cancer imaging and treatment. These micelles show enhanced efficacy against cancer cells while sparing normal cells.

Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Cancer Research

Background:

  • Developing effective drug delivery systems is crucial for cancer therapy.
  • Simultaneous imaging and treatment can improve therapeutic outcomes.
  • Novel anticancer agents require optimized delivery vehicles.

Purpose of the Study:

  • To develop fluorescent micellar carriers for controlled release of a novel anticancer drug.
  • To enable simultaneous intracellular imaging and cancer treatment.
  • To evaluate the efficacy and safety of drug-loaded nanomicelles.

Main Methods:

  • Synthesis of amphiphilic poly(acrylic acid)-block-poly(n-butyl acrylate) (PAA-b-PnBA) copolymer using Atom Transfer Radical Polymerization (ATRP).
  • Self-assembly of block copolymers to form nanosized micelles encapsulating a benzimidazole-hydrazone (BzH) anticancer drug.
  • Characterization of micelle properties (size, morphology, fluorescence) using DLS, TEM, and spectroscopy.
  • In vitro drug release studies and assessment of antiproliferative/cytotoxic effects on MDA-MB-231 (cancer) and MCF-10A (non-cancerous) cells.

Main Results:

  • Well-defined fluorescent nanomicelles with high encapsulation efficiency were successfully prepared.
  • Drug-loaded micelles demonstrated controlled release of the BzH drug over 72 hours.
  • BzH-loaded micelles exhibited enhanced antiproliferative and cytotoxic effects on MDA-MB-231 cells.
  • Micelles showed long-lasting effects on microtubule organization and induced apoptosis in cancer cells.
  • Minimal toxicity was observed on non-cancerous MCF-10A cells.

Conclusions:

  • Fluorescent nanomicellar carriers offer a promising platform for simultaneous cancer imaging and therapy.
  • The developed system enhances the efficacy of the novel BzH anticancer drug.
  • The targeted delivery and controlled release minimize side effects on healthy tissues.
Keywords:
benzimidazole derivativescytotoxicitydrug carriersdrug releasefluorescencemicellesnuclear and microtubule alterations

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