Abstract

The administration of drugs via transdermal therapeutic systems has become an attractive form of therapeutic approach, considering its advantages and the high patient compliance achieved, making them a viable alternative, especially in the treatment of chronic diseases. The purpose of our study was the development of polymer-based films containing tenoxicam (TX) and the analysis of dissolution kinetics. Auxiliary substances represent an important part of pharmaceutical forms, so during the first stage, TX and excipient compatibility were verified. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analyses were performed on TX and on physical mixtures of TX-HPMCE5 and TX-HPMC15kcP. Three polymeric films of TX (TX1, TX2, and TX3) were prepared using a solvent evaporation technique. Release studies were done at 32 °C ± 1 °C with a Franz diffusion cell. The results of the DSC and FT-IR analyses demonstrated the compatibility of the active substance with the two matrix-forming polymers. The results obtained in the release studies of TX from the proposed polymeric films suggested a pH-dependent behavior in all three polymeric films. At pH 5.5, flux values were between 8.058 ± 0.125 μg·cm−2·h−1 and 10.850 ± 0.380 μg·cm−2·h−1; and at pH 7.4, between 10.990 ± 0.2.490 μg·cm−2·h−1 and 53.140 ± 0.196 μg·cm−2·h−1. The Korsmeyer–Peppas model described a non-Fickian transport mechanism. The n values varied between 0.63–0.7 at pH 5.5 and 0.73–0.86 at pH 7.4, which suggested a diffusion depending on the matrix hydration and polymer relaxation.

Highlights

  • The lack of significant modification in the spectra confirmed the lack of interaction among TX and the excipients. This assumption was confirmed by the published data, which show the lack of any interaction of TX with polymers like hydroxypropyl methylcellulose

  • Similar results were published in 2015 by Ramkanth et al [24] concerning the incompatibilities of TX in hydroxypropyl methylcellulose (HPMC)-based films

  • We proposed the formulation and evaluation of three polymeric films containing TX

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Summary

Introduction

The physicochemical properties of active pharmaceutical ingredients lead to permeation of the skin barrier, and these ingredients are added to the barrier to external factors that the skin naturally manifests. This barrier, the stratum corneum, is the outermost layer of the skin, and is constituted of enucleated cells known as corneocytes. Ceramides, which belong to the class of sphingolipids, are responsible for forming structures capable of water fixation on their hydrophilic regions These structures encircle corneocytes, acting as an impermeable barrier with a natural moisturizing factor (NMF). They contain lipids, hydroxyl acids, amino acids, urea, and inorganic acids. The lipid content of the stratum corneum provides a low permeability for many external agents, and at the same time protects against them [1,2,3,4,5]

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