Department of Physical Chemistry and Biophysics, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211A, 55-556 Wroclaw, Poland.
Int J Mol Sci. 2023 Jan 31;24(3):2678. doi: 10.3390/ijms24032678.
Due to its high instability and rapid degradation under adverse conditions, tetracycline hydrochloride (TC) can cause difficulties in the development of an effective but stable formulation for the topical treatment of acne. The aim of the following work was to propose a hydrogel formulation that would ensure the stability of the antibiotic contained in it. Additionally, an important property of the prepared formulations was the activity of the alcoholamines contained in them against the components of the model sebum. This feature may help effectively cleanse the hair follicles in the accumulated sebum layer. A series of formulations with varying proportions of anionic polymer and alcoholamine and containing different polymers have been developed. The stability of tetracycline hydrochloride contained in the hydrogels was evaluated for 28 days by HPLC analysis. Formulations containing a large excess of TRIS alcoholamine led to the rapid degradation of TC from an initial concentration of about 10 µg/mL to about 1 µg/mL after 28 days. At the same time, these formulations showed the highest activity against artificial sebum components. Thanks to appropriately selected proportions of the components, it was possible to develop a formulation that assured the stability of tetracycline for ca. one month, while maintaining formulation activity against the components of model sebum.
由于盐酸四环素（TC）在不利条件下极不稳定且迅速降解，因此难以开发出有效且稳定的局部治疗痤疮的配方。以下工作的目的是提出一种水凝胶配方，以确保其中抗生素的稳定性。此外，所制备配方的一个重要特性是其中所含醇胺对模型皮脂成分的活性。这一特性可能有助于有效清除积聚皮脂层中的毛囊。已经开发了一系列含有不同比例阴离子聚合物和醇胺并含有不同聚合物的配方。通过 HPLC 分析评估了水凝胶中盐酸四环素的稳定性，为期 28 天。含有大量三羟甲基氨基甲烷醇胺的配方导致 TC 从初始浓度约 10 µg/mL 在 28 天后迅速降解至约 1 µg/mL。同时，这些配方对人工皮脂成分表现出最高的活性。通过适当选择各成分的比例，可以开发出一种能确保四环素稳定约一个月的配方，同时保持配方对模型皮脂成分的活性。
