In Vitro Development of Local Antiviral Formulations with Potent Virucidal Activity Against SARS-CoV-2 and Influenza Viruses.

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Juthaporn Ponphaiboon, Wantanwa Krongrawa, Sontaya Limmatvapirat, Sukannika Tubtimsri, Akanitt Jittmittraphap, Pornsawan Leaungwutiwong, Chulabhorn Mahidol, Somsak Ruchirawat, Prasat Kittakoop, Chutima Limmatvapirat
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Abstract

Background/Object: This study investigates the in vitro antiviral potential of D-limonene (DLM), monolaurin (ML), and cetylpyridinium chloride (CPC) in formulations targeting SARS-CoV-2 and influenza viruses. The aim was to develop oral and nasal formulations with optimized concentrations of these active ingredients to evaluate their efficacy, safety, and stability. Methods: Oral (formulation D) and nasal (formulation E) products were developed using specific concentrations of DLM (0.2-0.3% w/w), ML (0.1-0.2% w/w), and CPC (0.05-0.075% w/w). In vitro virucidal activity assays were conducted to assess the antiviral efficacy of the formulations against SARS-CoV-2 and influenza viruses. Stability testing was also performed under various storage conditions. Results: Formulation D (0.3% w/w DLM, 0.2% w/w ML, 0.05% w/w CPC, and 1.5% w/w Cremophor RH40) demonstrated a 3.875 ± 0.1021 log reduction and 99.99 ± 0.0032% efficacy against SARS-CoV-2 within 120 s. Formulation E (0.2% w/w DLM, 0.05% w/w CPC, and 0.75% w/w Cremophor RH40) showed a 2.9063 ± 0.1197 log reduction and 99.87 ± 0.0369% efficacy against SARS-CoV-2. Both formulations achieved >99.99% efficacy and log reductions exceeding 4.000 against various influenza strains. Stability testing confirmed optimal performance at 4 °C with no microbial contamination. Conclusions: The findings suggest that both formulations exhibit broad-spectrum antiviral activity against SARS-CoV-2 and influenza viruses in vitro. These results support their potential for further clinical evaluations and therapeutic applications, particularly in oral and nasal spray formulations.

对SARS-CoV-2和流感病毒具有有效抗病毒活性的局部抗病毒制剂的体外研制
背景/目的:研究d -柠檬烯(DLM)、单月桂素(ML)和氯化十六烷基吡啶(CPC)在SARS-CoV-2和流感病毒制剂中的体外抗病毒潜力。目的是开发具有这些活性成分的最佳浓度的口服和鼻制剂,以评估其功效,安全性和稳定性。方法:采用DLM (0.2-0.3% w/w)、ML (0.1-0.2% w/w)和CPC (0.05-0.075% w/w)的比浓度配制口服(D剂型)和鼻用(E剂型)制剂。通过体外杀病毒活性测定,评价制剂对SARS-CoV-2和流感病毒的抗病毒效果。并在不同的贮存条件下进行了稳定性试验。结果:配方D (0.3% w/w DLM, 0.2% w/w ML, 0.05% w/w CPC, 1.5% w/w Cremophor RH40)在120 s内对SARS-CoV-2的有效率为3.875±0.1021 log, 99.99±0.0032%。配方E (0.2% w/w DLM, 0.05% w/w CPC, 0.75% w/w Cremophor RH40)对SARS-CoV-2的疗效为2.9063±0.1197,有效率为99.87±0.0369%。两种配方均达到99.99%的功效,对各种流感毒株的对数减少超过4.000。稳定性测试证实在4°C下无微生物污染时性能最佳。结论:研究结果表明,这两种制剂在体外对SARS-CoV-2和流感病毒具有广谱抗病毒活性。这些结果支持其进一步临床评估和治疗应用的潜力,特别是在口服和鼻喷剂配方中。
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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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