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通过鼻腔给药的纳米结构微球黏附性输送白藜芦醇在鼻息肉模型小鼠。

Sinonasal Delivery of Resveratrol via Mucoadhesive Nanostructured Microparticles in a Nasal Polyp Mouse Model.

机构信息

Obstructive Upper airway Research (OUaR) Laboratory, Department of Pharmacology, Seoul National University College of Medicine, Seoul, 03080, Republic of Korea.

Department of Biomedical Science, Seoul National University Graduate School, Seoul, 03080, Republic of Korea.

出版信息

Sci Rep. 2017 Jan 10;7:40249. doi: 10.1038/srep40249.

Abstract

Resveratrol (RSV) has been shown to effectively suppress chronic rhinosinusitis with nasal polyps in a mouse model; however, when locally administered to the sinonasal cavity, bolus RSV is limited by low drug bioavailability owing to its low aqueous solubility and relatively rapid clearance from the administration site. To address this limitation, we propose mucoadhesive nanostructured microparticles (PLGA/PEG NM) as a potential carrier for the sinonasal delivery of RSV. In this study, PLGA/PEG NM released RSV in a sustained manner. Owing to the enlarged specific surface area of the nanostructures, PLGA/PEG NM had synergistically enhanced mucoadhesiveness and thus showed improved in vivo retention properties in the sinonasal cavity. Therefore, when tested in a mouse nasal polyp model, PLGA/PEG NM mitigated polyp formation and restored epithelial integrity better than the control treatments. The therapeutic effect was similar at half the dose of PLGA/PEG NM, suggesting improved local bioavailability of RSV in the sinonasal cavity.

摘要

白藜芦醇(RSV)已被证明可有效抑制鼻息肉慢性鼻窦炎的小鼠模型; 然而,当局部给药到鼻腔鼻窦腔,由于其低水溶性和从给药部位的相对快速清除,RSV 弹丸是受到低药物生物利用度的限制。为了解决这一限制,我们提出了作为 RSV 的经鼻给药的潜在载体的粘纳米结构微粒(PLGA/PEG NM)。在这项研究中,PLGA/PEG NM 以持续的方式释放 RSV。由于纳米结构的比表面积增大,PLGA/PEG NM 具有协同增强的粘膜粘附性,从而显示出在鼻腔鼻窦腔中改善的体内保留特性。因此,当在小鼠鼻息肉模型中进行测试时,PLGA/PEG NM 减轻了息肉形成并更好地恢复了上皮完整性,优于对照治疗。在 PLGA/PEG NM 的一半剂量下观察到相似的治疗效果,表明 RSV 在鼻腔鼻窦中的局部生物利用度得到了改善。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2973/5223156/d02d4b0c2f3b/srep40249-f1.jpg

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