The aim of this work was to test the in-vitro permeability of APIs (active pharmaceutical ingredients) across perforated and unperforated skin. Both, traditional adhesive matrices and hydrogel matrices were developed and tested. The result of this work is that it is possible to deliver model substances greater than 500Da through the skin barrier by perforating the epidermis.
Transdermal therapeutic systems (TTS) are dosage forms developed to transport an active pharmaceutical ingredient through the skin. This is done by applying a patch to the skin and is therefore a pain-free method. Since the establishment of this method, TTS have been a good alternative to traditional dosage forms such as tablets, injection needles and suppositories.
However, there is a crucial limit to TTS. APIs which are significantly greater than 500Da (500g/mol) cannot pass through the skin barrier. As several publications (cf. Cormier et al., 2004, Roxhed, 2007 and Yu et al., 2015) have shown, there is a possibility to transport APIs which are greater than 500Da through the skin. Combining TTS with microneedles (MN) is a way to produce microchannels through which the API can then pass the skin barrieCustomary MN systems were not sufficient to perforate the skin barrier. Hypodermic needles, however, are suitable to perforate the stratum corneum (SC). Consequently, the combination of TTS technology with MN technology is possible and should be further developed. Nevertheless, suitable MN have to be found. Hollow needles which are incorporated into a hydrogel matrix are a very promising option for a future product.
Inhaltsverzeichnis (Table of Contents)
- Introduction
- Theoretical background
- The barrier of the skin and transdermal therapeutic systems
- Transdermal therapeutic systems in combination with microneedles
- In-vitro skin permeation tests
- Materials and methods
- Chemicals and reagents
- Methods
- API coating
- Skin preparation
- Skin perforation
- Verifying the integrity and perforation of the skin
- Penetration assessment
- In-vitro skin permeation tests
- Statistical analysis
- Results
- Skin perforation tests
- In-vitro skin permeation tests
Zielsetzung und Themenschwerpunkte (Objectives and Key Themes)
This thesis explores the feasibility of developing innovative transdermal systems (TTS) for the delivery of active pharmaceutical ingredients (APIs) through the skin, specifically focusing on the use of microneedles (MN) to enhance skin permeability. The work aims to test the in-vitro permeability of APIs across perforated and unperforated skin using both traditional adhesive and hydrogel matrices.
- Investigating the potential of combining TTS with MN to overcome the skin barrier limitations for large APIs.
- Evaluating the effectiveness of MN in creating microchannels for enhanced API delivery through the skin.
- Comparing the permeability of APIs across perforated and unperforated skin using different matrix types.
- Assessing the suitability of different MN systems, including hypodermic needles, for skin perforation.
- Exploring promising future applications for TTS combined with MN, such as hollow needles incorporated into hydrogel matrices.
Zusammenfassung der Kapitel (Chapter Summaries)
- Introduction: This chapter provides a brief overview of the existing literature on transdermal therapeutic systems (TTS) and the limitations of delivering large APIs through the skin. It introduces the concept of combining TTS with microneedles (MN) as a potential solution to overcome these limitations.
- Theoretical background: This chapter presents a detailed discussion of the skin barrier, the mechanisms of drug delivery through the skin, and the use of MN for enhanced transdermal drug delivery. It also explains the principles of in-vitro skin permeation tests used in the study.
- Materials and methods: This chapter outlines the materials and methods used in the study, including the chemicals and reagents used, the preparation and perforation of skin samples, and the procedures for conducting in-vitro skin permeation tests.
- Results: This chapter presents the results of the skin perforation tests and in-vitro skin permeation tests, focusing on the effectiveness of different MN systems in perforating the skin and the permeability of APIs across perforated and unperforated skin.
Schlüsselwörter (Keywords)
This study focuses on transdermal drug delivery, microneedles, skin permeability, in-vitro permeation tests, active pharmaceutical ingredients, hydrogel matrices, and innovative transdermal systems. The research investigates the feasibility of using microneedles in combination with transdermal therapeutic systems to enhance the delivery of large APIs through the skin barrier. The research findings may have significant implications for the development of more effective and convenient drug delivery methods for a wider range of APIs.
- Quote paper
- Sebastian Kerski (Author), 2015, Feasibility Experiments for the Development of Innovative Transdermal Systems, Munich, GRIN Verlag, https://www.grin.com/document/946557