Title:Formulation Development and Evaluation of Apremilast Nanoemulgel for
Enhancing Permeability
Volume: 18
Issue: 2
Author(s): Neelam Patel*, Sunita Chaudhary and Ankit Chaudhary
Affiliation:
- Department of Pharmaceutics, SAL Institute of Pharmacy, Gujarat Technological University, Ahmedabad, Gujarat –
380060, India
Keywords:
Nanoemulgel, apremilast, carbopol, psoriasis, simple lattice design, skin permeation.
Abstract:
Background: Oral apremilast, a selective phosphodiesterase-4 inhibitor, is effective in the
treatment of moderate to severe plaque psoriasis and acute psoriatic arthritic disease. According to
BCS categorization, it is a class IV medication, which denotes low solubility and lesser permeability
through the skin.
Objective: The objective of the research is to develop a nanoemulsion that will increase apremilast’s
skin permeability. Utilizing a simplex lattice design, an optimised nanoemulsion has been developed,
and then transformed into a gel form and created as a nanoemulgel.
Methods: The nanoemulsion was developed by selecting the oil, surfactant, co-surfactant, and cosolvent,
in that order, based on the solubility study, and was then evaluated based on various criteria.
Different grades and concentrations of carbopol polymer were used to make nanoemulgel, which was
then tested for physicochemical parameters like pH, viscosity, spreadability, extrudability, percentage
of drug content, percentage of drug diffusion, skin permeation, and skin retention. For skin irritancy
tests, male Wistar albino rats weighing between 200 and 250 g were used to find out how likely it was
that apremilast-loaded nanoemulgel would cause skin irritation.
Results: The nanoemulsion formulation A5 containing 10% Captex 355 and 40% Smix in a 3:1 ratio
of Cremophore RH 40: Labrafil showed the smallest particle size and greatest drug diffusion. In comparison
to other formulations of emulgel, the 0.75 % concentration of carbopol 940 produced the best
results.
Conclusion: A stable nanoemulgel system with apremilast loaded was created, and a number of process
factors were assessed. The optimised batch produced repeatable results when evaluated, exhibited
no skin irritation, and was shown to be stable after three months at ambient conditions of temperature
and humidity.
