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Design, characterization, and biological evaluation of curcumin-loaded surfactant-based systems for topical drug delivery

机译:姜黄素负载型表面活性剂的局部给药系统的设计,表征和生物学评估

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摘要

From previous studies, it has been found that curcumin exhibits an anti-inflammatory activity and is being used for the treatment of skin disorders; however, it is hydrophobic and has weak penetrating ability, resulting in poor drug transport through the stratum corneum. The aim of this study was to develop liquid crystalline systems for topical administration of curcumin for the treatment of inflammation. These liquid crystalline systems were developed from oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol, and water as the surfactant, oil phase, and aqueous phase, respectively. These systems were characterized, and polarized light microscopy showed anisotropy with lamellar mesophases (Formulation 1) and hexagonal mesophases (Formulations 2 and 3), which were confirmed by the peak ratio measured using small-angle X-ray scattering. In addition, rheological tests revealed that the formulations exhibited gel-like behavior (G′>G″), as evidenced by the increased G′ values that indicate structured systems. Texture profile analysis showed that hexagonal mesophases have high values of hardness, adhesiveness, and compressibility, which indicate structured systems. In vitro studies on bioadhesion revealed that the hexagonal mesophases increased the bioadhesiveness of the systems to the skin of the pig ear. An in vivo inflammation experiment showed that the curcumin-loaded hexagonal mesophase exhibited an anti-inflammatory activity as compared to the positive control (dexamethasone). The results suggest that this system has a potential to be used as a bioadhesive vehicle for the topical administration of curcumin. Therefore, it is possible to conclude that these systems can be used for the optimization of drug delivery systems to the skin.
机译:从以前的研究中发现姜黄素具有抗炎活性,被用于治疗皮肤疾病。然而,它是疏水的并且具有弱的穿透能力,导致不良的药物通过角质层的运输。这项研究的目的是开发液晶系统,用于局部施用姜黄素治疗炎症。这些液晶系统分别由油酸,聚氧丙烯(5),聚氧乙烯(20)鲸蜡醇和作为表面活性剂的水,油相和水相开发而成。对这些系统进行了表征,并且偏光显微镜显示了层状中间相(配方1)和六角形中间相(配方2和3)的各向异性,这已通过使用小角度X射线散射测得的峰比得到证实。另外,流变学测试表明,制剂显示出凝胶状行为(G'> G''),如表明结构化系统的G'值增加所证明。纹理轮廓分析表明,六方中间相具有较高的硬度,粘合性和可压缩性值,表明结构化系统。体外生物粘附研究表明,六边形中间相增加了系统对猪耳皮肤的生物粘附性。体内炎症实验表明,与阳性对照(地塞米松)相比,姜黄素负载的六方中间相具有抗炎活性。结果表明该系统有潜力用作姜黄素局部给药的生物粘附载体。因此,可以得出结论,这些系统可以用于优化药物向皮肤的输送系统。

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