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Tazarotene-loaded in situ gels for potential management of psoriasis: biocompatibility, anti-inflammatory and analgesic effect.
Pharmaceutical Development and Technology ( IF 2.6 ) Pub Date : 2020-05-13 , DOI: 10.1080/10837450.2020.1765180
İpek Erol 1 , Neslihan Üstündağ Okur 2 , Duygu Orak 3, 4 , Hande Sipahi 3 , Ahmet Aydın 3 , Özgen Özer 1
Affiliation  

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 in situ gels for tazarotene skin delivery. The topical in situ gels were developed using thermosensitive poloxamers via cold method. They were examined for their appearance, sol-gel temperature, clarity, pH, viscosity, in vitro 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 E2 levels production in LPS-stimulated RAW264.7 murine macrophage cells. It was revealed that the in situ gels had no cytotoxic effect (∼95–100% cell viability) and nor irritation potential (∼97% cell viability), according to the in vitro EpiDerm™ reconstituted skin irritation test. Additionally, the 10% tazarotene-in situ gels showed possible analgesic activity since the production of prostaglandin E2 (PGE2) was decreased. In further, both concentrations of 5% and 10% tazarotene-in situ gels inhibited significantly the nitrite oxide production at 16% and 19%, respectively. Finally, the prepared in situ gels can act as a potential non-irritant alternative option for tazarotene topical skin delivery.



中文翻译:

负载他扎罗汀的原位凝胶可治疗牛皮癣:生物相容性,抗炎和镇痛作用。

牛皮癣是一种慢性自身炎性疾病,其特征是皮肤异常斑块。对于牛皮癣的治疗,建议使用局部类维生素A作为他扎罗汀。但是,他扎罗汀可能会刺激皮肤,从而限制了它的使用。在此,评估了原位凝胶用于他扎罗汀皮肤递送的可能用途。使用热敏泊洛沙姆通过冷方法开发了局部用原位凝胶。在体外检查了它们的外观,溶胶-凝胶温度,透明度,pH,粘度释放,稳定。通过研究它们的细胞毒性和刺激诱导能力来评估它们的生物相容性。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 2的水平来确定可能的抗炎和镇痛活性。根据体外EpiDerm™重构皮肤刺激试验,发现原位凝胶无细胞毒性作用(约95-100%细胞活力),也没有刺激潜力(约97%细胞活力)。此外,自生产前列腺素E 2(PGE 2)以来,10%的他扎罗汀原位凝胶显示出可能的止痛作用。)减少了。此外,浓度为5%和10%的他扎罗汀原位凝胶的浓度分别显着抑制了亚硝酸盐的产生,分别为16%和19%。最后,制备的原位凝胶可以作为他扎罗汀局部皮肤递送的潜在的非刺激性替代选择。

更新日期:2020-05-13
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