Abstract

Purpose: To design a transdermal norethisterone (NE) patch for controlled drug release Methods: Polymers, viz, sodium salt of carboxymethyl cellulose (CMCNa) and hydroxyethyl cellulose (HEC), as well as a plasticizer (propylene glycole, PG) were used at various ratios to prepare NE films. The drug was dispersed in water and mixed with the polymer gel/plasticizer mixture prior to film casting. Weight variation, thickness, tensile strength, and the interaction between drug and film excipient were evaluated. The films were also characterized by Fourier transform infrared spectroscopy (FT–IR). In vitro drug dissolution and release from the transdermal patches (coded C–L, C–T, H–L and H–T) were evaluated. Results: There was significant difference between the batches in terms of in vitro drug release (p > 0.05). Dissolved drug was significantly higher in H-T film when compared to C-L film (p < 0.05). İn addition, drug release was significantly higher from H-T patch than from C-L patch (p < 0.05). Conclusion: NE transdermal patches containing HEC and Transcutol® have been successfully formulated. They can potentially be used to deliver NE via transdermal route to decrease the side effects associated with the oral route of administration of the hormone. Keywords: Norethisterone, Transdermal delivery, Controlled release, Hormone therapy

Highlights

  • Norethisterone (NE) is a potent synthetic progestogen which is used for the treatment of dysfunctional bleeding by shifting the time of menstruation [1,2]

  • Drugs can be avoided from the first pass metabolism, thereby increasing their bioavailability [6,7]

  • This study was aimed at preparing transdermal patches of NE for the first time, in order to overcome the side effects associated with oral administration of the drug

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Summary

Introduction

Norethisterone (NE) is a potent synthetic progestogen which is used for the treatment of dysfunctional bleeding by shifting the time of menstruation [1,2]. Transdermal therapeutic systems (TTS) are developed for administration of drugs that have short plasma half-lives through the skin, so as to achieve controlled release. These systems minimize systemic side effects such as gastrointestinal (GI) side effects of drugs when taken through the oral route. Drugs can be avoided from the first pass metabolism, thereby increasing their bioavailability [6,7]. Another advantage is that trans-dermal drugs can be removed by the patient when necessary. TTS, can be prepared using either natural or synthetic polymers in membrane or matrix systems [8,9]

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