Title:Implementing Central Composite Design for Developing Transdermal Diacerein-Loaded Niosomes: Ex vivo Permeation and In vivo Deposition
Volume: 15
Issue: 9
Author(s): Diana Edwar Aziz, Aly Ahmed Abdelbary*Abdelhalim Ibrahim Elassasy
Affiliation:
- Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo,Egypt
Keywords:
Diacerein, central composite, niosomes, optimization, ex vivo permeation, skin deposition studies.
Abstract: Background: Niosomes are surfactant-based vesicular nanosystems that proved their efficiency
in transdermal delivery by overcoming skin inherent anatomic barrier; startum corneum. Central
composite design is an efficient tool for developing and optimizing niosomal formulations using fewer
experiments.
Objective: The objective of this study was to prepare niosomes as a transdermal delivery system of
diacerein using film hydration technique, employing central composite design, for avoiding its oral
gastrointestinal problems.
Methods: Three-level three-factor central composite design was employed for attaining optimal
niosomes formulation with the desired characteristics. Three formulation variables were assessed:
amount of salt in hydration medium (X1), lipid amount (X2) and number of surfactant parts (X3). DCNloaded
niosomes were evaluated for entrapment efficiency percent (Y1), particle size (Y2), polydispersity
index (Y3) and zeta potential (Y4). The suggested optimal niosomes were subjected to further characterization
and utilized as a nucleus for developing elastic vesicles for comparative ex vivo and in vivo
studies.
Results: The values of the independent variables (X1, X2 and X3) in the optimal niosomes formulation
were 0 g, 150 mg and 5 parts, respectively. It showed entrapment efficiency percentage of 95.63%,
particle size of 436.65 nm, polydispersity index of 0.47 and zeta potential of -38.80 mV. Results of ex
vivo permeation and skin deposition studies showed enhanced skin permeation and retention capacity of
the prepared vesicles than drug suspension.
Conclusion: Results revealed that a transdermal niosomal system was successfully prepared and evaluated
using central composite design which will result in delivering diacerein efficiently, avoiding its
oral problems.