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姜黄素传递体负载温敏型鼻内原位凝胶作为 SARS-CoV-2 的新型抗病毒治疗策略。

Curcumin Transferosome-Loaded Thermosensitive Intranasal in situ Gel as Prospective Antiviral Therapy for SARS-Cov-2.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Deraya University, Minia, Egypt.

出版信息

Int J Nanomedicine. 2023 Oct 17;18:5831-5869. doi: 10.2147/IJN.S423251. eCollection 2023.

DOI:10.2147/IJN.S423251
PMID:37869062
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10590117/
Abstract

PURPOSE

Immunomodulatory and broad-spectrum antiviral activities have motivated the evaluation of curcumin for Coronavirus infection 2019 (COVID-19) management. Inadequate bioavailability is the main impediment to the therapeutic effects of oral Cur. This study aimed to develop an optimal curcumin transferosome-loaded thermosensitive in situ gel to improve its delivery to the lungs.

METHODS

Transferosomes were developed by using 3 screening layouts. The phospholipid concentration as well as the concentration and type of surfactant were considered independent variables. The entrapment efficiency (EE%), size, surface charge, and polydispersity index (PDI) were regarded as dependent factors. A cold technique was employed to develop thermosensitive in-situ gels. Optimized transferosomes were loaded onto the selected gels. The produced gel was assessed based on shape attributes, ex vivo permeability enhancement, and the safety of the nasal mucosa. The in vitro cytotoxicity, antiviral cytopathic effect, and plaque assay (CV/CPE/Plaque activity), and in vivo performance were evaluated after intranasal administration in experimental rabbits.

RESULTS

The optimized preparation displayed a particle size of 664.3 ± 69.3 nm, EE% of 82.8 ± 0.02%, ZP of -11.23 ± 2.5 mV, and PDI of 0.6 ± 0.03. The in vitro curcumin release from the optimized transferosomal gel was markedly improved compared with that of the free drug-loaded gel. An ex vivo permeation study revealed a significant improvement (2.58-fold) in drug permeability across nasal tissues of sheep. Histopathological screening confirmed the safety of these preparations. This formulation showed high antiviral activity against SARS-CoV-2 at reduced concentrations. High relative bioavailability (226.45%) was attained after the formula intranasally administered to rabbits compared to the free drug in-situ gel. The curcumin transferosome gel displayed a relatively high lung accumulation after intranasal administration.

CONCLUSION

This study provides a promising formulation for the antiviral treatment of COVID-19 patients, which can be evaluated further in preclinical and clinical studies.

摘要

目的

免疫调节和广谱抗病毒活性促使人们评估姜黄素用于 2019 年冠状病毒病（COVID-19）管理。口服姜黄素的生物利用度不足是其治疗效果的主要障碍。本研究旨在开发一种最佳的姜黄素转体负载温敏原位凝胶，以改善其向肺部的递药。

方法

通过使用 3 种筛选设计来开发转体。将磷脂浓度以及表面活性剂的浓度和类型视为独立变量。包封效率（EE%）、粒径、表面电荷和多分散指数（PDI）被视为依赖因素。采用冷技术开发温敏原位凝胶。将优化后的转体加载到选定的凝胶上。根据形状属性、体外透皮增强作用以及鼻黏膜的安全性来评估所产生的凝胶。在实验兔中经鼻给药后，评估体外细胞毒性、抗病毒细胞病变效应和噬菌斑分析（CV/CPE/Plaque activity）以及体内性能。

结果

优化后的制剂显示出 664.3 ± 69.3nm 的粒径、82.8 ± 0.02%的 EE%、-11.23 ± 2.5mV 的 ZP 和 0.6 ± 0.03 的 PDI。与游离药物负载凝胶相比，优化后的转体凝胶中姜黄素的体外释放明显改善。体外透皮研究表明，药物透过绵羊鼻组织的渗透性显著提高（2.58 倍）。组织病理学筛选证实了这些制剂的安全性。该配方在降低浓度下对 SARS-CoV-2 表现出高抗病毒活性。与游离药物原位凝胶相比，该配方经兔鼻腔给药后获得了较高的相对生物利用度（226.45%）。姜黄素转体凝胶经鼻腔给药后肺部蓄积较高。

结论

本研究为 COVID-19 患者的抗病毒治疗提供了一种有前途的配方，可在临床前和临床研究中进一步评估。

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