Title:Preparation and Optimization of Controlled Release Nanoparticles Containing Cefixime Using Central Composite Design: An Attempt to Enrich
Its Antimicrobial Activity
Volume: 19
Issue: 3
Author(s): Mohammad Ali Mahjoub, Pedram Ebrahimnejad*, Fatemeh Shahlaee, Pouneh Ebrahimi and Zaynab Sadeghi-Ghadi
Affiliation:
- Pharmaceutical Sciences Research Center, Hemoglobinopathy Institute, Mazandaran University of Medical Sciences,
Sari, Iran
- Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
Keywords:
Nanoparticles, chitosan, cefixime, central composite, antibacterial activity, safety.
Abstract: Background: Due to the increased resistance against existing antibiotics, research is essential
to discover new and alternative ways to control infections induced by resistant pathogens.
Objective: The goal of the current scrutinization was to enrich the dissolution rate and antibacterial
property of cefixime (CEF) orally.
Methods: To achieve the desired results, chitosan nanoparticles (NPs) containing CEF were fabricated
using the ionic gelation method. Central Composite design has been applied to get the optimal
formulation for the delivery of CEF. The effect of three variables, such as the concentration of
chitosan, tripolyphosphate, and tween 80, on the characteristics of NPs was evaluated.
Results: The optimized NPs involved a relatively monodispersed size distribution with an average
diameter of 193 nm and a zeta potential of about 11 mV. The scanning tunneling microscope confirmed
the size of NPs. The surface morphology of NPs was observed by scanning electron microscopy.
The calorimetric analysis indicated the amorphous state of cefixime in the formulation. The
dissolution rate of NPs in aqueous media was acceptable and the model of release kinetics for CEF
from NPs followed the Peppas model. The potency of CEF in NPs against various types of bacteria
was hopefully efficient. The ex-vivo release study demonstrated higher penetration of NPs from the
rat intestine compared to free drug. The cell culture study showed the safety of the optimized formulation.
Conclusion: Chitosan NPs could be considered a significant system for the controlled delivery of
CEF due to its antibacterial effectiveness.