Development of a transcutaneous form of desloratadine

Valentin P. Ageev; Andrey V. Zaborovskiy; Dina V. Yunina; Larisa A. Tararina; Mikhail K. Devkota; Dmitry N.  Andreev; Aleksandra E. Pyanzina; Vasilisa I. Shlyapkina; Yulia A. Buldygina; Oleg A. Kulikov; Nikolay A. Pyataev

doi:10.18413/rrpharmacology.10.487

Authors

Valentin P. Ageev National Research Ogarev Mordovia State University https://orcid.org/0000-0001-5152-5358
Andrey V. Zaborovskiy Russian University of Medicine of the Ministry of Health of the Russian Federation https://orcid.org/0000-0002-7923-9916
Dina V. Yunina Russian University of Medicine of the Ministry of Health of the Russian Federation https://orcid.org/0000-0001-8901-9557
Larisa A. Tararina Russian University of Medicine of the Ministry of Health of the Russian Federation https://orcid.org/0000-0001-8006-698X
Mikhail K. Devkota Russian University of Medicine of the Ministry of Health of the Russian Federation https://orcid.org/0000-0002-3736-4196
Dmitry N. Andreev Russian University of Medicine of the Ministry of Health of the Russian Federation https://orcid.org/0000-0002-4007-7112
Aleksandra E. Pyanzina National Research Ogarev Mordovia State University, 68 Bolshevistskaya St., Saransk, Republic of Mordovia 430005 Russia https://orcid.org/0009-0007-2090-3249
Vasilisa I. Shlyapkina 1National Research Ogarev Mordovia State University https://orcid.org/0000-0002-5248-0136
Yulia A. Buldygina National Research Ogarev Mordovia State University https://orcid.org/0009-0003-8930-1749
Oleg A. Kulikov National Research Ogarev Mordovia State University https://orcid.org/0000-0003-4411-677X
Nikolay A. Pyataev National Research Ogarev Mordovia State University https://orcid.org/0000-0002-9688-7640

DOI:

https://doi.org/10.18413/rrpharmacology.10.487

Abstract

Introduction: For people with allergies, it is not always possible to prevent allergens admission to the body. For this reason, it is essential to create a long-acting drug that can prevent an allergic reaction. The very promising option is a transdermal therapeutic system (TTS), with H1 blockers. The aim of the study: To create a technology for the production of desloratadine-based TTS, suitable for routine use with prolonged drug releasing.

Materials and Methods: Polyvinylpyrrolidone K30 (PVP) was used as the main matrix polymer for TTS, and the Kruofilm polymer membrane was used as the adhesive layer. The formation of the polymer membrane was carried out by drying a water-alcohol solution of the components at a temperature of 60ºC. Characterization of the obtained dosage forms was made by spectrophotometry. The resulting micelles size was measured by dynamic light scattering.

Results and Discussion: Round shaped TTS (patches) with water-dissolved DL and its micellar form were obtained. The size of micelles with DL was 22.8±5.2 nm. The spectrophotometric method for determining DL has been developed. The containing of DL in the patches ranged from 5 to 25 mg per patch, depending on the manufacturing technology.

Conclusion: We have developed TTSs containing DL by a solution and a micellar form. A top adhesive layer has been selected that has moisture resistance, strength and reliable fixation of the matrix with the active substance on the skin. A method for the spectrophotometric determination of DL in solutions and patches was developed and validated.

Graphical Abstract

Keywords:

allergy, desloratadine, transdermal therapeutic system, patch, micelles

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Author Contribution

Valentin P. Ageev, National Research Ogarev Mordovia State University

Head of the Educational and Scientific Laboratory for Preclinical and Clinical Trials of Targeted Forms of Pharmaceuticals (Federal Center for the Development of Biotechnology and Medicine) National Research Mordovia State University, Saransk, Russia; e-mail: valeageev@yandex.ru; ORCID ID https://orcid.org/0000-0001-5152-5358. Developing the experiment design, conducting the experiment, analyzing literary data, and writing the text of the article.

Andrey V. Zaborovskiy, Russian University of Medicine of the Ministry of Health of the Russian Federation

Dr. Habil. Med., Associate Professor, Head of the Department of Pharmacology, Russian University of Medicine, Moscow, Russia; e-mail: azabor@mail.ru; ORCID ID https://orcid.org/0000-0002-7923-9916. Developing the experiment design, analyzing literary data. and writing the text of the article.

Dina V. Yunina, Russian University of Medicine of the Ministry of Health of the Russian Federation

Lecturer, Department of Pharmacology, Russian University of Medicine? Moscow, Russia; e-mail: yunina@msmsu.ru; ORCID ID https://orcid.org/0000-0001-8901-9557. Developing the experiment design, analyzing literary data, and writing the text of the article.

Larisa A. Tararina, Russian University of Medicine of the Ministry of Health of the Russian Federation

Senior Lecturer, Department of Pharmacology, Russian University of Medicine, Moscow, Russia; e-mail: 79104906528@yandex.ru; ORCID ID https://orcid.org/0000-0001-8006-698X. Developing the experiment design, conducting the experiment, analyzing literary data, and writing the text of the article.

Mikhail K. Devkota, Russian University of Medicine of the Ministry of Health of the Russian Federation

Lecturer, Department of Pharmacology, Russian University of Medicine, Mpscow, Russia; e-mail: devkota@bk.ru; ORCID ID https://orcid.org/0000-0002-3736-4196. Developing the experiment design, conducting the experiment, analyzing literary data, and writing the text of the article.

Dmitry N. Andreev, Russian University of Medicine of the Ministry of Health of the Russian Federation

Ph.D. of Medical Sciences, Assistant Professor, Department of Propaedeutics of Internal Diseases and Gastroenterology, Faculty of Medicine, Scientific Research Institute of Clinical Medicine named after N.A. Semashko, Russian University of Medicine, Moscow, Russia; e-mail: dna-mit8@mail.ru; ORCID ID https://orcid.org/0000-0002-4007-7112. А nalyzing literary data and writing the text of the article.

Aleksandra E. Pyanzina, National Research Ogarev Mordovia State University, 68 Bolshevistskaya St., Saransk, Republic of Mordovia 430005 Russia

Laboratory assistant, Department of Anesthesiology, Intensive Care and Transfusiology with a course in Disaster Medicine, National Research Mordovia State University, Saransk, Russia; e-mail: PyanzinaSSS@yandex.ru; ORCID ID https://orcid.org/0009-0007-2090-3249. Developing the experiment design, analyzing literary data, and writing the text of the article. Conducting the experiment, analysis of clinical manifestations, and statistical analysis of the data.

Vasilisa I. Shlyapkina, 1National Research Ogarev Mordovia State University

Junior researcher, Educational and Scientific Laboratory for Preclinical and Clinical Trials of Targeted Forms of Pharmaceuticals (Federal Center for the Development of Biotechnology and Medicine) National Research Mordovia State University, Saransk, Russia; e-mail: shlyapkina.98@mail.ru; ORCID ID https://orcid.org/0000-0002-5248-0136. Conducting the experiment, analyzing clinical manifestations, and conducting thestatistical analysis of the data.

Yulia A. Buldygina, National Research Ogarev Mordovia State University

Assistant Director, Federal Center for the Development of Biotechnology and Medicine, National Research Mordovia State University, Saransk, Russia; e-mail: yulia.buldygina@yandex.ru; ORCID ID https://orcid.org/0009-0003-8930-1749. Conducting the experiment, analyzing clinical manifestations, and conducting the statistical analysis of the data.

Oleg A. Kulikov, National Research Ogarev Mordovia State University

Doct. Sci. Medicine, Assistant Professor, Department of Anesthesiology, Reanimatology and Transfusiology with a course in Disaster Medicine, National Research Mordovia State University, Saransk, Russia; e-mail: oleg-kulikov-84@mail.ru; ORCID ID https://orcid.org/0000-0003-4411-677X. Drawing up a research plan and providing the general guidance, developing the design of the experiment, analyzing literary data, and writing the text of the article.

Nikolay A. Pyataev, National Research Ogarev Mordovia State University

Doct. Sci. Medicine, Assistant Professor, Head of the Federal Center for the Development of Biotechnology and Medicine, National Research Mordovia State University, Saransk, Russia; e-mail: pyataevna@mail.ru; ORCID ID https://orcid.org/0000-0002-9688-7640. Drawing up a research plan and providing the general guidance, developing the design of the experiment, analyzing literary data, and writing the text of the article.