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Encapsulation and Sustained Release of Curcumin using Superparamagnetic Silica Reservoirs

机译:姜黄素的包封和缓释使用超顺磁性二氧化硅储层

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Curcumin is a yellow polyphenol found in the rhizomes of the plant Curcuma longa. The compound has shown promise towards wound healing, which is attributed to the presence of myofibroblast, and in enhancing fibronectin and collagen expression.[1] The treatment of wounds with curcumin has been reported to increase the formation of granulation tissue, which includes greater cellular content; neo-vascularisation; and faster re-epithelialisation of wounds.[2] These findings suggest that curcumin may be able to improve radiation- induced wound repair delay. Curcumin has also been reported to show antioxidant,[3] anti-inflammatory,[4] antimicrobial,[ 5] and anticancer capability.[6] Various animal models or human studies also showed that curcumin is extremely safe even at a dosage as high as 12 g per day.[7] However, all of the above-mentioned properties of curcumin are yet to be fully realised, due to its low water solubility, fast degradation, and poor bioavailability. Oral administration of curcumin at a dose of 2 gkg1 to rats, only resulted in a maximum serum concentration of 1.35 (0.23 mgmL1 after approximately 1 h, whereas in humans the same dose of curcumin resulted in either undetectable or extremely low (0.005 mgmL1 at 1 h) serum levels.[8] Attempts have been made to encapsulate curcumin in polymeric micelles, lipidbased nanoparticles, and hydrogels in order to improve its water solubility, stability, and bioavailability.[9] However, organic- based carriers such as polymeric nanoparticles, liposomes, and micelles are shown to suffer from poor stability owing to biochemical attack and swelling.[10] On the other hand, silica-based drug-delivery carriers are chemically and thermally more stable, highly hydrophilic, and biocompatible. Furthermore, the high density of silanol groups located at the silica surface (pores and external surface) can be readily treated with coupling agents to provide sites for tethering specific bioactive substrates including antibodies.[11]
机译:姜黄素是一种黄色的多酚,存在于植物姜黄的根茎中。该化合物显示出对伤口愈合的希望,这归因于成肌纤维细胞的存在,并有助于增强纤连蛋白和胶原蛋白的表达。[1]据报道用姜黄素治疗伤口会增加肉芽组织的形成,包括更多的细胞含量。新血管形成;更快地重新上皮伤口。[2]这些发现表明姜黄素可能能够改善辐射引起的伤口修复延迟。姜黄素也据报道显示出抗氧化剂,[3]抗炎,[4]抗菌,[5]和抗癌能力。[6]各种动物模型或人体研究还表明,即使每天使用多达12克的剂量,姜黄素也是极其安全的。[7]然而,由于姜黄素的低水溶性,快速降解和不良的生物利用度,姜黄素的所有上述特性尚未得到充分实现。向大鼠口服姜黄素2 gkg1的剂量仅导致最高血清浓度为1.35(约1小时后为0.23 mgmL1,而在人类中,相同剂量的姜黄素则导致检测不到或极低(1时为0.005 mgmL1) h)血清水平。[8]尝试将姜黄素包封在聚合物胶束,脂质基纳米颗粒和水凝胶中,以提高其水溶性,稳定性和生物利用度。[9]然而,有机基载体如聚合物纳米颗粒[10]另一方面,基于二氧化硅的药物递送载体在化学和热方面更稳定,高度亲水性和生物相容性,因此它们的稳定性受到不良影响。[10]位于二氧化硅表面(孔和外表面)的高密度硅烷醇基团可以很容易地用偶联剂处理,以提供用于束缚特定生物活性底物的位点,包括抗体。[11]

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