Evaluation of antimicrobial properties and antioxidant activity of rosmarinic acid loaded Resomer RG 502 H based nanoparticles against tert-butyl hydroperoxide-induced oxidative stress: A detailed formulation, characterization and efficacy determination study

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY Journal of Drug Delivery Science and Technology Pub Date : 2025-04-01 Epub Date: 2025-02-17 DOI:10.1016/j.jddst.2025.106721
Büşra Solak , Pervin Soyer , Elif Kaya-Tilki , A. Alper Öztürk
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Abstract

This study investigates the innovative application of rosmarinic acid (RA)-loaded Resomer RG 502 H-based nanoparticles (NPs) in enhancing therapeutic efficacy against oxidative stress and microbial infections. Rosmarinic acid, a natural polyphenol with significant pharmacological properties, has demonstrated potential in treating various diseases, including cancer, diabetes, and inflammatory disorders. However, its clinical utility is hampered by poor water solubility and bioavailability. To address these challenges, we employed a nanoprecipitation technique to create biodegradable PLGA-based NPs that encapsulate RA effectively. The formulation showed uniformity with a particle size of 217.7 nm ± 4.3 and a PDI of 0.129 ± 0.007. A study was conducted with trehalose to ensure stability during storage. The resultant NPs not only exhibit high encapsulation efficiency (≈72.8 %) but also provide sustained release profiles for 72 h, which are crucial for maximizing RA's therapeutic effects. DSC, FT-IR, and 1H-NMR analyses confirmed the encapsulation and structural integrity of the formulation. Pharmacological evaluations, including the effects of RA and B-RA-NP on NIH/3T3 cell viability, the evaluation of optimal tBHP concentration, and exposure time for assessing antioxidant activity, reveal that these NPs significantly enhance the antioxidant activity of RA while exhibiting potent antimicrobial effects against a spectrum of pathogenic microorganisms. By leveraging nanotechnology for drug delivery, we present a promising strategy to improve the bioavailability and efficacy of RA, thus advancing its application in therapeutic formulations. The findings underscore the transformative potential of nanotechnology in enhancing the clinical relevance of natural compounds, paving the way for novel therapeutic strategies in pharmaceutical applications.

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迷迭香酸负载Resomer RG 502h纳米颗粒抗叔丁基过氧化氢氧化应激的抗菌性能和抗氧化活性评价:详细的配方、表征和药效测定研究
本研究探讨了迷迭香酸(RA)负载Resomer RG 502 h基纳米颗粒(NPs)在抗氧化应激和微生物感染方面的创新应用。迷迭香酸是一种天然多酚,具有重要的药理特性,在治疗多种疾病,包括癌症、糖尿病和炎症性疾病方面具有潜力。然而,它的临床应用受到水溶性和生物利用度差的阻碍。为了解决这些挑战,我们采用纳米沉淀技术来创建可生物降解的基于plga的NPs,有效地封装RA。该配方均匀,粒径为217.7 nm±4.3,PDI为0.129±0.007。为了确保海藻糖在贮存期间的稳定性,对海藻糖进行了研究。所得到的NPs不仅具有较高的包封效率(≈72.8%),而且具有72小时的缓释特性,这对于最大化RA的治疗效果至关重要。DSC, FT-IR和1H-NMR分析证实了该制剂的包封性和结构完整性。药理学评估,包括RA和B-RA-NP对NIH/3T3细胞活力的影响,最佳thbhp浓度评估和抗氧化活性评估的暴露时间,表明这些NPs显著增强RA的抗氧化活性,同时对一系列致病微生物表现出强大的抗菌作用。通过利用纳米技术给药,我们提出了一种有希望的策略来提高RA的生物利用度和疗效,从而推进其在治疗配方中的应用。这些发现强调了纳米技术在增强天然化合物临床相关性方面的变革潜力,为药物应用中的新治疗策略铺平了道路。
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来源期刊
CiteScore
8.00
自引率
8.00%
发文量
879
审稿时长
94 days
期刊介绍: The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.
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