Objective:
The aim of the present study was to design nanocarriers for the topical application
of rivastigmine.
Methods:
The effect of cosurfactants, hydrophilic gel and loading amount on the permeability of rivastigmine
through rat skin was evaluated. Skin irritation tests and stability tests were performed to
evaluate the utility of tested formulations.
Results:
The results showed that the microemulsion formation and characteristics of drug-loaded formulations
were related to many parameters of the components. When using microemulsion systems as
a vehicle, the permeation rate remarkably increased about 13.2~24.3-fold and the lag time was significantly
shortened from 24 h to 4.7 h. Formulations containing a cosurfactant of Diethylene Glycol
Monobutyl Ether (DEGBE) showed higher enhancement effect, while increasing the loading dose from
0.5% to 5% further increased the flux about 2.1-fold and shortened the lag time.
Conclusion:
The drug-loaded experimental formulation did not cause skin irritation and had good stability
at 20ºC and 40ºC storage for at least 3 months. The result showed that gel-based microemulsion
formulation could be a promising approach for topical administration.
