Title:Fabrication and Optimization of Electrospun Polymeric Nanofibers
Loaded with 5-Fluorouracil and Rosemary Extract
Volume: 10
Issue: 3
Author(s): Reza Jamali, Erfaneh Ghassami*, Masoud Sadeghi Dinani, Razieh Ghasemi and Mina Mirian
Affiliation:
- Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University
of Medical Sciences, Isfahan, Iran
Keywords:
5-fluorouracil, rosemary extract, electrospinning, polymeric nanofibers, transdermal drug delivery, PVA.
Abstract:
Background: Topical 5-fluorouracil (5FU) is one of the most prescribed medications
for different types of skin cancer; however, it is associated with drug resistance and adverse effects.
Rosemary extract has promising dose-dependent antitumor effects, as well as a synergistic
effect in combination with 5-fluorouracil, besides sensitization of the 5-FU-resistant cells.
Objective: Polymeric nanofibers loaded with 5FU and rosemary extract were optimized to combine
both ingredients in one controlled release drug delivery system, aiming to enhance the efficacy
while retaining the adverse effects.
Methods: Polymeric nanofibers loaded with 5-FU and rosemary were fabricated via electrospinning
technique. Design expert software was utilized to study the effect of independent variables,
including polymer concentration, voltage, and feeding rate on the characteristics of the resulting
nanofibers. Afterwards, the FTIR spectrum and release kinetic of the drug and extract from the
optimized nanofibers and their cytotoxic effect against A375 cell line were investigated.
Results: The formulation composed of 6.65% PVA electrospun at 1 mL.h-1 and 17.5kV was chosen
as the optimum fabrication condition. The mean diameter of the optimized nanofibers was 755
nm. The drug and rosemary extract contents were 75.38 and 93.42%, respectively. The fabrication
yield was 100%, bioadhesion force was 1.28 N, and bead abundance was 10 per field. The cytotoxicity
of the optimized formulation was significantly higher than the control groups.
Conclusion: According to the appropriate loading percentage, release efficiency and release kinetics,
bioadhesion force, and cytotoxicity, these nanofibers could be further investigated as a topical
treatment option to increase the efficacy of 5-FU.
