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