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Sustained release of prednisone and mesalamine from diatom exoskeletons : bioinspiration for the development of safe oral drug delivery devices to tackle gastrointestinal diseases

机译:硅藻外骨骼中泼尼松和美沙拉敏的持续释放:生物灵感开发安全的口服药物递送装置以应对胃肠道疾病

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摘要

Mesoporous silicon and silica-based particles have recently been synthesized and proposed forthe controlled delivery of several drugs [1,2]. On the other hand, nature and in particular marineorganisms have been the source and inspiration for the development of different biomedicalapplications, including drug delivery devices [3]. On the border of both rests diatomsexoskeletons, nature-made porous silica-based microparticles with amazing morphologicalfeatures, promising a high potential in drug delivery. Nevertheless, its safety and drugpermeability on oral formulations have not yet been studied. In this study, we have demonstratedthat diatoms silica microparticles (DSM) have almost no toxicity in colon cancer cells Caco-2, HT-29, HCT-116 and Caco-2/HT-29, even at concentrations as high as 1000 μg/mL. Moreover, thedelivery profile of two common drugs to address gastrointestinal diseases, mesalamine (antiinflammatory)and prednisone (glucocorticosteroid). DSMs are able to release prednisone in acontrolled manner and change its absorption pattern, which may improve the safety of itsadministration. In addition, DSMs can enhance the permeation of mesalamine. These resultsconfirm the potential of DSMs for the development of oral formulations for the therapy ofgastrointestinal diseases.
机译:最近已经合成了介孔硅和二氧化硅基颗粒,并提出可控制地输送几种药物[1,2]。另一方面,自然界,特别是海洋生物,已成为包括药物输送装置在内的各种生物医学应用发展的源泉和灵感[3]。在两个硅藻骨架的边界,硅藻土是天然制造的多孔二氧化硅基微粒,具有令人惊叹的形态特征,有望在药物输送中发挥巨大潜力。然而,尚未研究其在口服制剂上的安全性和药物渗透性。在这项研究中,我们证明了硅藻硅微粒(DSM)对结肠癌细胞Caco-2,HT-29,HCT-116和Caco-2 / HT-29几乎没有毒性,即使浓度高达1000μg/毫升此外,用于治疗胃肠道疾病的两种常用药物,美沙拉敏(抗炎药)和泼尼松(糖皮质激素)的给药方式。 DSM能够以受控方式释放泼尼松并改变其吸收方式,从而可以提高其给药的安全性。此外,DSM可以增强美沙拉敏的渗透性。这些结果证实了帝斯曼在开发用于治疗胃肠道疾病的口服制剂方面的潜力。

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