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载有还原氧化石墨烯的水凝胶经皮传递丁丙诺啡治疗骨关节炎。

Transdermal delivery of buprenorphine from reduced graphene oxide laden hydrogel to treat osteoarthritis.

机构信息

First Department of Orthopedics, Baoji Gaoxin People's Hospital, Baoji City, Shaanxi Province, China.

出版信息

J Biomater Sci Polym Ed. 2021 May;32(7):874-885. doi: 10.1080/09205063.2021.1877065. Epub 2021 Feb 11.

DOI:10.1080/09205063.2021.1877065
PMID:33570467
Abstract

The patients with chronic pain in osteoarthritis often have insufficient pain relief from non-opioids analgesics. Buprenorphine is a promising molecule for symptomatic relief of chronic pain. The marketed parenteral injections and sublingual tablets have short duration of action (half-life = 2.7 h), which is not suitable to manage chronic pain. The purpose of this research was to design buprenorphine-loaded Pluronic F127-reduced graphene oxide transdermal (noninvasive) hydrogel to achieve sustained release of buprenorphine to manage chronic pain in osteoarthritis. Pluronic F127 was used to stabilize the reduced graphene oxide in hydrogel system. The characterization studies including Fourier transform infrared spectroscopy, X-ray diffraction, and Raman spectroscopy confirmed the synthesis of Pluronic F127-reduced graphene oxide from graphite. The transmission electron microscopy image showed flat nanosheets of reduced graphene oxide (rGO). The developed hydrogel showed desirable pH, viscosity, adhesiveness, hardness, and cohesiveness for transdermal application. The release study demonstrated the ability of the Pluronic F127-reduced graphene oxide (P-rGO) hydrogel to prolong release up to 14 days, owing to the strong π-π interactions between the graphene oxide (GO) and the buprenorphine. In cold ethanol tail flick model, the GO hydrogel showed sustained analgesic effect in comparison with hydrogel without rGO. Thus, this study demonstrated the potential of using Pluronic F127-reduced graphene oxide nanocarriers to prolong local analgesia for effective management for chronic pain.

摘要

骨关节炎慢性疼痛患者常因非阿片类镇痛药而无法充分缓解疼痛。丁丙诺啡是一种有前途的治疗慢性疼痛症状的分子。市售的注射剂和舌下片剂作用持续时间短(半衰期=2.7 小时),不适合治疗慢性疼痛。本研究旨在设计丁丙诺啡负载的 Pluronic F127 还原氧化石墨烯经皮(非侵入性)水凝胶,以实现丁丙诺啡的持续释放,从而治疗骨关节炎的慢性疼痛。Pluronic F127 用于稳定水凝胶系统中的还原氧化石墨烯。傅里叶变换红外光谱、X 射线衍射和拉曼光谱等表征研究证实了从石墨合成了 Pluronic F127 还原氧化石墨烯。透射电子显微镜图像显示了还原氧化石墨烯(rGO)的扁平纳米片。所开发的水凝胶具有理想的 pH 值、粘度、粘附性、硬度和内聚性,适合经皮应用。释放研究表明,Pluronic F127 还原氧化石墨烯(P-rGO)水凝胶具有长达 14 天的延长释放能力,这是由于氧化石墨烯(GO)和丁丙诺啡之间的强π-π相互作用。在冷乙醇尾部摆动模型中,GO 水凝胶与不含 rGO 的水凝胶相比表现出持续的镇痛作用。因此,本研究表明,使用 Pluronic F127 还原氧化石墨烯纳米载体延长局部镇痛时间对于有效治疗慢性疼痛具有潜力。

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