Transdermal Delivery of Antipsychotics: Rationale and Current Status

The aim of this article is to provide the rationale for the development of transdermal formulations of antipsychotics by highlighting their main advantages, starting with an overview of the antipsychotic formulations that are currently available on the market. Progress regarding transdermal antipsychotic formulations was investigated by performing a search of papers, patents and clinical trials published in the last 10 years. Available data on antipsychotic transdermal formulations are reported and discussed, focusing on the characteristics of the dosage forms and their ability to promote drug absorption. Despite the current availability of a large number of antipsychotics, only a few of these drugs (e.g. aripiprazole, asenapine, blonanserin, chlorpromazine, haloperidol, olanzapine, prochlorperazine, quetiapine, and risperidone) have been developed as transdermal delivery systems. Several papers and patents show that transdermal formulations, such as creams, films, gels, nanosystems, patches, solutions, and sprays, have been evaluated with the aim of expanding the clinical utility of antipsychotic drugs. In particular, the employment of different strategies, such as the use of nanoparticles/vesicles, or permeation enhancers as well as microneedles with iontophoresis, may improve the absorption of antipsychotic drugs through the skin. However, few clinical trials on transdermal delivery of antipsychotic drugs are available and only delivery systems containing asenapine and blonanserin have shown interesting clinical results in terms of pharmacokinetic data, efficacy, and tolerability. Recently, the transdermal patch formulation of blonanserin was approved in Japan for the treatment of schizophrenia.