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. 2024 Feb 7;29(4):767.
doi: 10.3390/molecules29040767.

Establishment and Validation of a Transdermal Drug Delivery System for the Anti-Depressant Drug Citalopram Hydrobromide

Yi-Yang Sun  1 , Ya-Jing Ni  1 , Run-Jia Wang  1 , Zi-Cheng Qin  1 , Zhao Liu  2 , Li-Hui Xiao  2 , Yan-Qiang Liu  1
Affiliations

Establishment and Validation of a Transdermal Drug Delivery System for the Anti-Depressant Drug Citalopram Hydrobromide

Yi-Yang Sun et al. Molecules. .

Abstract

To enhance the bioavailability and antihypertensive effect of the anti-depressant drug citalopram hydrobromide (CTH) we developed a sustained-release transdermal delivery system containing CTH. A transdermal diffusion meter was first used to determine the optimal formulation of the CTH transdermal drug delivery system (TDDS). Then, based on the determined formulation, a sustained-release patch was prepared; its physical characteristics, including quality, stickiness, and appearance, were evaluated, and its pharmacokinetics and irritation to the skin were evaluated by applying it to rabbits and rats. The optimal formulation of the CTH TDDS was 49.2% hydroxypropyl methyl cellulose K100M, 32.8% polyvinylpyrrolidone K30, 16% oleic acid-azone, and 2% polyacrylic acid resin II. The system continuously released an effective dose of CTH for 24 h and significantly enhanced its bioavailability, with a higher area under the curve, good stability, and no skin irritation. The developed CTH TDDS possessed a sustained-release effect and good characteristics and pharmacokinetics; therefore, it has the potential for clinical application as an antidepressant.

Keywords: citalopram hydrobromide; pharmacokinetics; skin irritation; transdermal delivery.

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Conflict of interest statement

Authors Zhao Liu and Li-hui Xiao were employed by the Harvest Pharmaceutical Co., Ltd. The remaining authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.

Figures

Figure 1
Figure 1
Effect of the excipient material ratio on the in vitro release of CTH from the transdermal drug delivery system. Data are presented as the mean ± standard deviation (SD; n = 3). The marked different letters indicate significant difference among treatments. CTH, citalopram hydrobromide.
Figure 2
Figure 2
Effect of the penetration enhancer concentration on the in vitro release of CTH from the transdermal drug delivery system. Data are presented as the mean ± SD (n = 3). The marked different letters indicate significant difference between treatments, and the same letters indicate no significant difference between treatments.
Figure 3
Figure 3
Effect of polyacrylic acid resin II on the in vitro release of CTH from the transdermal drug delivery system. Data are presented as the mean ± SD (n = 3). The marked different letters indicate significant difference between treatments, and the same letters indicate no significant difference between treatments.
Figure 4
Figure 4
SEM image of the CTH transdermal drug delivery system. SEM: scanning electron microscopy. The images showed that the patch had good integrity and the drugs were evenly distributed in the polymer matrix.
Figure 5
Figure 5
Plasma drug concentration–time curve analysis in rabbits after the administration of CTH via the transdermal drug delivery system and oral application. Data are presented as the mean ± SD (n = 6). * p < 0.05, vs. the oral administration group.
Figure 6
Figure 6
Skin irritation study of the CTH transdermal drug delivery system. (A1–F1): Before application of the patch; (A2–F2): after removal of the patch.
Figure 7
Figure 7
SEM images of the skin after transdermal administration of CTH. (A1–C1): Before application of the patch; (A2–C2): after removal of the patch. Images showed that the surface structure and morphology of the skin did not significantly change after the transdermal administration of CTH.
See this image and copyright information in PMC

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