β-cyclodextrin/alginate nanoparticles encapsulated 5-fluorouracil as an effective and safe anticancer drug delivery system

Abstract

Although 5-Fluorouracil (5-FU) is one of the most frequently used cytotoxic chemotherapy drugs in the treatment of cancer, it possesses a short biological half-life and toxic side effects against normal healthy cells. In this work, β-cyclodextrin/alginate (β-CD/Alg) nanoparticles loaded with 5-fluorouracil (5-FU) were prepared to evaluate release properties and bioactivity in different pH media. Stable nanocomposites with the best loading efficiency (36%) and encapsulation efficiency (90%) were successfully fabricated. The size of the nanocomposite solution was determined via dynamic light scattering (DLS) to be in the range 30–120 nm with a mean size of 70 nm, while TEM images showed the particle size of the nanocomposite to be in the range 30–80 nm with a mean size of 50 nm. The release profile of 5-FU in a simulated gastric fluid (pH 1.2) was much lower than in a simulated colorectal fluid (pH 7.4). The release behaviour of 5-FU from the nanocomposite was confirmed by the change in morphology in the pH media. A cytotoxicity assay indicated that the nanocomposite is an effective delivery system for 5-FU with strong antiproliferative activity against MCF-7 cells and negligible effects on normal healthy cells.

Keywords

• Ionotropic gelation
• Anticancer
• β-cyclodextrin
• Alginate
• 5-fluorouracil
• Drug delivery