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评估纳米脂质体 Arthrocen(NANOCEN)局部用药对小鼠的抗炎和镇痛作用。

Estimation of Anti-inflammatory and Analgesic Effects of Topical NANOCEN (Nanoliposomal Arthrocen) on Mice.

机构信息

Division of Research and Development, Pharmin USA, LLC, San Jose, California, USA.

Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

AAPS PharmSciTech. 2019 Jun 24;20(6):233. doi: 10.1208/s12249-019-1445-5.

Abstract

The purpose of this study was to evaluate the effect of topical application of nanoliposomal avocado/soybean unsaponifiables (NANOCEN) on inflammation inhibition and pain relief in mice. NANOCEN was prepared by the injection method and characterized for vesicle size, charge, entrapment efficiency, in vitro release, and 1-month vesicle stability. The analysis of ASU formulation showed that liposomes had an average size of around 146 nm with a surface charge of - 43 mV. SEM and TEM imaging confirmed the spherical shape of the nanovesicles in ASU formulation. Moreover, ASU nanoliposomes had a high entrapment efficiency (96%) and exhibited significantly (p < 0.0001) sustained release of the drug in vitro model. The topical NANOCEN (ASU 2%) showed robust anti-inflammatory (p < 0.01) and analgesic effect (p < 0.01) superior to ibuprofen 5%. The histopathology of the inflamed tissues confirmed that the topical ASU formulation potentially (p < 0.001) inhibited infiltration of inflammatory cells. Our findings suggest that the topical formulation of NANOCEN may have local applications for pain relief in medicine.

摘要

本研究旨在评估纳米脂体鳄梨/大豆不皂化物(NANOCEN)局部应用对抑制炎症和缓解疼痛的作用。通过注射法制备 NANOCEN,对其进行了囊泡大小、电荷、包封效率、体外释放和 1 个月囊泡稳定性的特征分析。ASU 制剂的分析表明,脂质体的平均粒径约为 146nm,表面电荷为-43mV。SEM 和 TEM 成像证实了 ASU 制剂中纳米囊泡的球形形状。此外,ASU 纳米脂质体具有高包封效率(96%),并在体外模型中表现出显著(p<0.0001)的药物持续释放。局部 NANOCEN(ASU 2%)表现出强大的抗炎(p<0.01)和镇痛效果(p<0.01),优于布洛芬 5%。炎症组织的组织病理学证实,局部 ASU 制剂可能潜在地(p<0.001)抑制了炎症细胞的浸润。我们的研究结果表明,NANOCEN 的局部制剂可能在医学领域具有缓解疼痛的局部应用。

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