Kostrzębska Agnieszka, Szczepaniak Gabriela
Department of Physical Chemistry and Biophysics, Faculty of Pharmacy, Wroclaw Medical University, Poland.
Polim Med. 2024 Jul-Dec;54(2):155-159. doi: 10.17219/pim/196256.
Acne vulgaris is a common inflammatory skin condition affecting almost 85% of the adolescent and young adult population. The etiopathogenesis of this dermatosis involves an imbalance in the skin microbiome, leading to inflammation of both the skin and hair follicles.
The aim of this study was to develop topical anti-acne formulations with increased therapeutic efficacy and reduced risk of developing antibiotic resistance. Six hydrogel formulations containing azelaic acid or its derivative, azeloglycine, in combination with tetracycline hydrochloride were prepared as part of the study.
The investigated formulations were prepared using an Eprus U500 pharmaceutical mixer and the pH was determined using an ERH-11S electrode designed for dense substances and a CPC-505 Elmetron pH-meter. The formulations were analyzed for tetracycline stability in the presence of additional active ingredients and varying pH over a period of 35 days using high-performance liquid chromatography (HPLC). In addition, the effects of azeloglycine and azelaic acid on the viscosity of the prepared formulations were evaluated using a Brookfield DV2T rotational viscometer.
Chromatographic analysis showed significant stability of tetracycline in most formulations, with azeloglycine-containing formulations showing less degradation of the antibiotic than azelaic acid-containing preparations. In addition, azeloglycine-containing gels exhibited more favorable rheological properties, which may facilitate better application and be more beneficial to patients.
The results suggest that formulations containing azeloglycine and tetracycline may be a promising strategy for acne therapy, offering increased tetracycline stability and an optimal rheological profile, which may result in prolonged therapeutic effect and more effective drug delivery to the skin.
寻常痤疮是一种常见的炎症性皮肤病,几乎影响85%的青少年和青年人群。这种皮肤病的发病机制涉及皮肤微生物群失衡,导致皮肤和毛囊炎症。
本研究的目的是开发具有更高治疗效果和降低抗生素耐药性风险的局部抗痤疮制剂。作为研究的一部分,制备了六种含有壬二酸或其衍生物壬二酰甘氨酸并与盐酸四环素联合的水凝胶制剂。
使用Eprus U500制药混合器制备所研究的制剂,并使用专为浓稠物质设计的ERH - 11S电极和CPC - 505 Elmetron pH计测定pH值。使用高效液相色谱法(HPLC)在35天的时间内分析制剂在存在其他活性成分和不同pH值情况下四环素的稳定性。此外,使用Brookfield DV2T旋转粘度计评估壬二酰甘氨酸和壬二酸对所制备制剂粘度的影响。
色谱分析表明,大多数制剂中四环素具有显著稳定性,含壬二酰甘氨酸的制剂中抗生素的降解比含壬二酸的制剂少。此外,含壬二酰甘氨酸的凝胶表现出更有利的流变学性质,这可能便于更好地应用且对患者更有益。
结果表明含壬二酰甘氨酸和四环素的制剂可能是痤疮治疗的一种有前景的策略,具有提高四环素稳定性和优化的流变学特性,这可能导致治疗效果延长以及药物向皮肤的递送更有效。