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Тhe article presents the theoretical justification for the choice of active pharmaceutical ingredients of antihypertensive action for the creation of new forms of delivery – transdermal therapeutic systems. The aim: monitoring of studies on the use of angiotensin-converting enzyme (ACE) inhibitors in the development of transdermal drugs for the treatment of hypertension. Materials: open access electronic resources of scientific periodicals from around the world: Google Scholar (https:// scholar.google.com/); PubMed (https://pubmed.ncbi.nlm.nih.gov/); Sciencedirect (https://www.sciencedirect.com/); Pubchem (https://pubchem.ncbi.nlm.nih.gov/); National Library of Ukraine named after V. I. Vernadskyi (http:// www.nbuv.gov.ua/); Ukrainian Institute of Intellectual Property (Ukrpatent) (https://sis.ukrpatent.org/uk/); Industrial Property (https://base.uipv.org/searchBul/); USPTO. The United States Patent and Trademark Office (https://www. uspto.gov/patents/search); European Patent Office (EPO) (https://www.epo.org/). Methods of the research: information search, theoretical analysis and systematization of data from scientific sources, logical analysis. Results: a review of scientific sources was carried out, and an analysis of ACE inhibitors as candidates for the creation of transdermal forms for the treatment of arterial hypertension was carried out. The pharmacological and physicochemical aspects of the possibility of their use for introduction through the skin are defined. It has been established that the search and development of the latest means of treatment of arterial hypertension, which would significantly increase the duration and quality of life of patients, are extremely relevant. Transdermal drug delivery systems are one of the pharmaceutical products being developed on the world market, and their use allows overcoming the associated disadvantages of other delivery routes. Conclusions: the review of domestic and foreign literature confirmed the relevance of biopharmaceutical research in the field of development of innovative dosage forms – transdermal therapeutic systems for the treatment of hypertension. The choice of promising antihypertensive active pharmaceutical ingredients of the ACE group (enalapril maleate, lisinopril dihydrate, and captopril) is substantiated, taking into account their specific physicochemical properties that are suitable for penetration through the skin. The market for transdermal drug delivery is increasing, and there is a prospect of higher growth rates in this market in the coming years. [ABSTRACT FROM AUTHOR]