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Updated: Jun 12, 2026

Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
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Cyclodextrin-Based Nanocarriers for 5-Fluorouracil: Cholesteryl Modification Enhances Antitumor Activity Against

Beata Skonieczna1, Bartosz Maliszewski2,3, Natalia Wasiluk1

  • 1Department of Experimental Pharmacology, Medical University of Bialystok, Bialystok, Poland.

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Cholesterol-modified cyclodextrin (CD21chol) enhances 5-fluorouracil (5-FU) anticancer activity. The 1:3 CD21chol:5-FU complex shows potent cytotoxicity against colorectal cancer cells with minimal impact on healthy cells, indicating therapeutic promise.

Keywords:
5-fluorouracilcholesterol moietycolorectal cancerdrug delivery systemsβ-cyclodextrin

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Area of Science:

  • Nanotechnology in drug delivery
  • Cancer therapeutics
  • Pharmacology

Background:

  • Cholesterol-modified cyclodextrin (CD21chol) as a drug delivery vehicle.
  • 5-fluorouracil (5-FU) is a common chemotherapeutic agent.
  • Investigating novel formulations to enhance 5-FU efficacy and reduce toxicity.

Purpose of the Study:

  • To evaluate the biological activity of cholesterol-modified cyclodextrin (CD21chol) complexes with 5-fluorouracil (5-FU).
  • To determine the optimal molar ratio for potent anticancer formulation.
  • To assess the safety profile of these complexes in non-cancerous cells.

Main Methods:

  • Preparation of CD21chol:5-FU inclusion complexes at molar ratios of 1:1, 1:2, and 1:3.
  • Characterization of physicochemical properties including zeta potential and particle size.
  • In vitro evaluation of cytotoxicity, metabolic activity, membrane integrity, and apoptosis in DLD-1 colorectal cancer cells and control cell lines.

Main Results:

  • The 1:3 CD21chol:5-FU complex exhibited enhanced physicochemical stability and the strongest cytotoxic effect on DLD-1 cells.
  • Significant reduction in cell viability and metabolic activity (>60%) and activation of apoptosis pathways (caspases 3/7, 8, 9) were observed.
  • Minimal toxicity was noted in non-tumorigenic fibroblasts and cardiomyocytes.

Conclusions:

  • CD21chol-based delivery systems significantly improve the anticancer efficacy of 5-FU.
  • The 1:3 CD21chol:5-FU complex is a promising candidate for colorectal cancer therapy development.