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用于局部给药的载姜黄素表面活性剂基体系的设计、表征及生物学评价。

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

作者信息

Fonseca-Santos Bruno, Dos Santos Aline Martins, Rodero Camila Fernanda, Gremião Maria Palmira Daflon, Chorilli Marlus

机构信息

School of Pharmaceutical Sciences, UNESP - São Paulo State University, Araraquara, São Paulo Brazil.

出版信息

Int J Nanomedicine. 2016 Sep 8;11:4553-4562. doi: 10.2147/IJN.S108675. eCollection 2016.

Abstract

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.

摘要

从先前的研究中发现,姜黄素具有抗炎活性,正被用于治疗皮肤疾病;然而,它具有疏水性且穿透能力较弱,导致药物透过角质层的运输效果不佳。本研究的目的是开发用于局部给药姜黄素以治疗炎症的液晶系统。这些液晶系统分别由油酸、聚氧丙烯(5)聚氧乙烯(20)十六醇以及水作为表面活性剂、油相和水相来制备。对这些系统进行了表征,偏光显微镜显示出层状中间相(制剂1)和六方中间相(制剂2和3)的各向异性,这通过小角X射线散射测量的峰比得到证实。此外,流变学测试表明这些制剂表现出凝胶状行为(G' > G″),G'值的增加表明系统具有结构化,这证明了这一点。质地剖面分析表明六方中间相具有较高的硬度、粘性和可压缩性值,这表明系统具有结构化。体外生物粘附研究表明六方中间相增加了系统对猪耳皮肤的生物粘附性。一项体内炎症实验表明,与阳性对照(地塞米松)相比,负载姜黄素的六方中间相表现出抗炎活性。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,这些系统可用于优化皮肤给药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8046/5019438/9e48b6e258f5/ijn-11-4553Fig1.jpg

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