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Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel

机译:通过制剂加入姜黄素抗炎作用的增强在乳糜碱基纳米杆菌中

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摘要

Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm2·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug.
机译:背景:姜黄素(CUR)具有各种有益的药理学性质,包括抗氧化剂,抗菌剂,抗癌和抗炎活动。然而,低水溶性和随后的生物利用度大大限制了其有效性。此外,最近证明了Myrrh油作为治疗炎症障碍的精油的作用。目前调查的目的是通过开发Cur纳米杆菌来提高Cur功效,这有助于改善其透皮递送的溶解度和渗透性。方法:评价配制的制剂(Cur凝胶,肌胶和纳米肺泡),用于它们的物理外观,铺展性,粘度,粒度,体外释放和离体渗透研究。使用角叉菜胶诱导的大鼠后爪水肿方法估计体内抗炎活性。结果:配方的CUR负载制剂表现出良好的物理特性,其在可接受的透皮制剂范围内。 12小时后从凝胶,肌凝胶和纳米液中释放来自凝胶,emulcel和纳米杆菌,分别为72.17±3.76,51.93±3.81和62.0±3.9%。当配制到纳米杆胶中时,Cur的皮肤渗透显着(p <0.05),因为它显示出具有最高增强比(ER)的最佳稳态透皮通量(SSTF)值(108.6±3.8μg/ cm 2·h)(7.1± 0.2)。体内抗炎研究证明,CUR负载的纳米杆胶显示出最低溶胀的百分比(12小时后26.6%)。结论:所获得的数据证实了纳米杆菌剂型的潜力,并建立了MyRRH油的协同作用和Cur作为先进的抗炎药。

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