Faculty of Pharmacy, Department of Pharmaceutical Technology, Ege University, Izmir, Turkey.
Faculty of Pharmacy, Department of Pharmaceutical Technology, University of Health Sciences, Istanbul, Turkey.
Pharm Dev Technol. 2020 Oct;25(8):909-918. doi: 10.1080/10837450.2020.1765180. Epub 2020 May 13.
Psoriasis is a chronic autoinflammatory disorder characterized by patches of abnormal skin. For psoriasis management, the application of topical retinoids as Tazarotene is recommended. However, Tazarotene could induce skin irritation limiting its use. Herein, it is evaluated the possible usage of gels for tazarotene skin delivery. The topical gels were developed using thermosensitive poloxamers via cold method. They were examined for their appearance, sol-gel temperature, clarity, pH, viscosity, release, and stability. Their biocompatibility was evaluated by investigating their cytotoxicity and irritation inducing capacity. The possible anti-inflammatory and analgesic activities were determined by measuring the nitric oxide and prostaglandin E levels production in LPS-stimulated RAW264.7 murine macrophage cells. It was revealed that the gels had no cytotoxic effect (∼95-100% cell viability) and nor irritation potential (∼97% cell viability), according to the EpiDerm™ reconstituted skin irritation test. Additionally, the 10% tazarotene- gels showed possible analgesic activity since the production of prostaglandin E (PGE) was decreased. In further, both concentrations of 5% and 10% tazarotene- gels inhibited significantly the nitrite oxide production at 16% and 19%, respectively. Finally, the prepared gels can act as a potential non-irritant alternative option for tazarotene topical skin delivery.
银屑病是一种慢性自身炎症性疾病，其特征是出现异常皮肤斑块。对于银屑病的管理，建议应用局部维甲酸，如他扎罗汀。然而，他扎罗汀可能会引起皮肤刺激，限制其使用。在此，评估了将他扎罗汀凝胶用于皮肤递送的可能性。通过冷法使用热敏性泊洛沙姆制备局部凝胶。对其外观、溶胶-凝胶温度、透明度、pH 值、粘度、释放和稳定性进行了考察。通过研究细胞毒性和诱导刺激能力来评估其生物相容性。通过测量 LPS 刺激的 RAW264.7 鼠巨噬细胞中一氧化氮和前列腺素 E 水平的产生来确定其可能的抗炎和镇痛活性。根据 EpiDerm™重建皮肤刺激性试验，结果表明，凝胶没有细胞毒性（约 95-100%细胞活力），也没有刺激潜力（约 97%细胞活力）。此外，10%他扎罗汀凝胶显示出可能的镇痛活性，因为前列腺素 E (PGE) 的产生减少。此外，浓度为 5%和 10%的 5%和 10%他扎罗汀凝胶分别抑制了 16%和 19%的亚硝酸盐氧化产物的产生。最后，所制备的凝胶可作为局部皮肤递送他扎罗汀的潜在非刺激性替代选择。
