Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127, Bologna, Italy.
CNS Drugs. 2019 Sep;33(9):849-865. doi: 10.1007/s40263-019-00659-7.
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.
本文旨在通过概述目前市场上可获得的抗精神病药物制剂，突出其主要优势，为抗精神病药物经皮制剂的开发提供理论依据。通过对过去 10 年发表的论文、专利和临床试验进行检索，研究了经皮抗精神病药物制剂的进展。报告和讨论了抗精神病药物经皮制剂的现有数据，重点关注剂型的特点及其促进药物吸收的能力。尽管目前有大量的抗精神病药物，但只有少数几种药物（例如阿立哌唑、阿塞那平、布南色林、氯丙嗪、氟哌啶醇、奥氮平、奋乃静、喹硫平和利培酮）已被开发为经皮给药系统。许多论文和专利表明，已经评估了经皮制剂，如乳膏、薄膜、凝胶、纳米系统、贴片、溶液和喷雾剂，旨在扩大抗精神病药物的临床应用。特别是，采用不同策略，如使用纳米颗粒/囊泡或渗透增强剂以及带有离子电渗疗法的微针，可能会改善抗精神病药物经皮吸收。然而，关于抗精神病药物经皮给药的临床试验很少，只有包含阿塞那平和布南色林的给药系统在药代动力学数据、疗效和耐受性方面显示出有趣的临床结果。最近，布南色林经皮贴片制剂在日本获得批准，用于治疗精神分裂症。
