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丝素纳米粒用于塞来昔布和姜黄素的递送:在骨关节炎体外模型中的 ROS 清除和抗炎活性。

Silk fibroin nanoparticles for celecoxib and curcumin delivery: ROS-scavenging and anti-inflammatory activities in an in vitro model of osteoarthritis.

机构信息

University of Pavia, Department of Drug Sciences, 27100 Pavia, Italy.

University of Pavia, Department of Drug Sciences, 27100 Pavia, Italy; Pharmaexceed srl, 27100 Pavia, Italy.

出版信息

Eur J Pharm Biopharm. 2019 Apr;137:37-45. doi: 10.1016/j.ejpb.2019.02.008. Epub 2019 Feb 14.

Abstract

This paper aims at demonstrating silk fibroin nanoparticles (SFNs) promote anti-inflammatory properties of celecoxib (CXB) or curcumin (CUR), and could be exploited for osteoarthritis (OA) treatment. Nanoparticles were prepared by desolvation method and physico-chemically characterized (FT-IR, DSC, TGA, SEM, size distribution and drug release); empty and drug loaded nanoparticles were tested for their ROS-scavenging activity, hemolytic properties, cytotoxicity, and anti-inflammatory potency in an OA in vitro model. Results indicate that a controlled drug release has been achieved by varying the drug loading. Curcumin plus SFNs exhibited a synergistic antioxidant effect, while CXB was, in some manner, inhibitory. Both free drugs resulted highly cytotoxic while cell viability reached high values when encapsulated in SFNs. No appreciable differences in anti-inflammatory activity was evidenced between CUR loaded SFNs and CXB. In conclusion, SFNs is an optimal carrier to improve cyto- and hemo-compatibility of both CUR and CXB.

摘要

本文旨在展示丝素纳米颗粒(SFNs)可促进塞来昔布(CXB)或姜黄素(CUR)的抗炎特性,并可用于骨关节炎(OA)的治疗。通过去溶剂法制备纳米颗粒,并对其进行物理化学性质表征(傅里叶变换红外光谱、差示扫描量热法、热重分析、扫描电子显微镜、粒径分布和药物释放);测试空纳米颗粒和载药纳米颗粒的 ROS 清除活性、溶血特性、细胞毒性以及在 OA 的体外模型中的抗炎效果。结果表明,通过改变药物载药量可实现药物的控制释放。姜黄素加丝素纳米颗粒表现出协同抗氧化作用,而 CXB 在某种程度上具有抑制作用。游离药物的细胞毒性很高,而包封在 SFNs 中的药物则具有很高的细胞活力。负载 CUR 的 SFNs 和 CXB 的抗炎活性之间没有明显差异。总之,SFNs 是一种可改善 CUR 和 CXB 的细胞和血液相容性的理想载体。

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