Wojtyłko Monika, Nowicka Ariadna B, Froelich Anna, Szybowicz Mirosław, Banaszek Tobiasz, Tomczak Dorota, Kuczko Wiesław, Wichniarek Radosław, Budnik Irena, Jadach Barbara, Kordyl Oliwia, Białek Antoni, Krysztofiak Julia, Osmałek Tomasz, Lamprou Dimitrios A
3D Printing Division, Chair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, Poland.
Doctoral School, Poznan University of Medical Sciences, 70 Bukowska Street, 60-812 Poznań, Poland.
Molecules. 2025 Jan 15;30(2):322. doi: 10.3390/molecules30020322.
Agomelatine (AGM) is an effective antidepressant with low oral bioavailability due to intensive hepatic metabolism. Transdermal administration of agomelatine may increase its bioavailability and reduce the doses necessary for therapeutic effects. However, transdermal delivery requires crossing the barrier. For this purpose, the use of microneedles may increase the efficiency of administration. The aim of this study was to prepare an agomelatine-loaded hydrogel suitable for coating microneedles for the transdermal drug delivery of AGM. The optimized formulations were subjected to spectroscopic and rheological characterization and mechanical tests, as well as tested for release through an artificial membrane and permeation through human skin ex vivo. Both hydrogels were found to have suitable parameters for coating microneedles using the dip-coating method, including the stability of the substance at the process temperature, shear-thinning behavior, and appropriate textural parameters such as adhesion or hardness. Additionally, two formulations were tested for potential application to the skin alone because the gels showed suitable mechanical properties for the skin application. In this case, the ethanol gel was characterized by higher skin permeability and better spreadability. The information obtained in this study will allow the preparation of coated microneedles for the transdermal administration of agomelatine.
阿戈美拉汀（AGM）是一种有效的抗抑郁药，但由于肝脏的高强度代谢，其口服生物利用度较低。阿戈美拉汀的透皮给药可能会提高其生物利用度，并减少达到治疗效果所需的剂量。然而，透皮给药需要穿过屏障。为此，使用微针可能会提高给药效率。本研究的目的是制备一种适合包被微针用于阿戈美拉汀透皮给药的载阿戈美拉汀水凝胶。对优化后的制剂进行了光谱和流变学表征、力学测试，并测试了其通过人工膜的释放和离体人皮肤的渗透情况。发现两种水凝胶都具有使用浸涂法包被微针的合适参数，包括该物质在加工温度下的稳定性、剪切变稀行为以及诸如粘附性或硬度等合适的质地参数。此外，还测试了两种制剂单独用于皮肤的潜在应用，因为这些凝胶显示出适合用于皮肤的力学性能。在这种情况下，乙醇凝胶的特点是皮肤渗透性更高且铺展性更好。本研究中获得的信息将有助于制备用于阿戈美拉汀透皮给药的包被微针。
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