Aims: Biodegradable polymeric microneedles containing atorvastatin calcium were developed
in order to improve the percutaneous absorption of the drug, useful for the treatment of hypercholesterolemia.
Background: The use of physical enhancers like microneedles have shown good results to increase the
delivery of drugs through the skin, the use of microneedles has very important advantages for transdermal
drug delivery, for example, they are painless, easy to use and safe, they increase time interval
of drug activity, dose, and reductions in adverse reactions, they also offer, the facility to remove the
system instantly of the skin.
Objective: Develop polymer microneedles loaded with a calcium atorvastatin and evaluate them by
Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), bioadhesion, postwetting-
bioadhesion, breaking strength, drug release test and in vitro percutaneous absorption studies
to demonstrate the use of microneedles atorvastatin is able to cross the skin.
Methods: The microneedles were made with poly (methyl vinyl ether-alt-maleic acid) as biodegradable
polymer using the technique of casting in solution in a mold. After solidification these microneedles
were characterized by Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy
(SEM), bioadhesion, post-wetting-bioadhesion, breaking strength, drug release test and in vitro percutaneous
Results: In general, the performances were satisfactory for optimal formulation in terms of DSC with
no interactions between drug and excipients, SEM shows microneedles with a conical shape, bioadhesion
of 1570 g.f, post wetting-bioadhesion of 1503.4 g.f, breaking strength of 1566.7g.f that is sufficient
to disrupt Stratum corneum, good drug release and a flux of 33.4 μg/cm2*h with a tLag of 15.14
h for the in vitro percutaneous absorption.
Conclusion: The results indicate that it is possible to generate microneedles to increase the percutaneous
absorption of calcium atorvastatin transdermally, with the potential to be used as an alternative to
the oral route for the treatment of dyslipidemias.