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载有松萝酸的有前途的纳米凝胶用于口腔溃疡治疗:在兔子中的开发、表征和评价。

Promising nanogels loaded with usnic acid for oral ulcer treatment: development, characterization, and evaluation in rabbits.

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Technology, Ege University, Bornova, Izmir, Turkey.

Faculty of Pharmacy, Department of Pharmaceutical Technology, University of Health Sciences, Uskudar, Istanbul, Turkey.

出版信息

Pharm Dev Technol. 2021 Apr;26(4):431-443. doi: 10.1080/10837450.2021.1885441. Epub 2021 Feb 22.

Abstract

This study aimed to present an effective formulation targeting oral ulcers that will remain in the application site for a longer period, reducing the frequency of administration. As a candidate formulation, usnic acid (UA) was loaded into the optimum nanogels. The characterization studies included physical, rheological, and bioadhesive properties as well as release and studies. The rheological results revealed that the nanogels present pseudoplastic flow behavior. drug release showed a prolonged pattern. In further, the chosen UA nanogels showed very low percentages of penetration and permeation. F13, which showed the highest release, suitable bioadhesive properties (0.475 ± 0.033 N/cm) and eligible particle size (250.22 ± 4.11 nm), PDI (0.089 ± 0.052), and zeta potential (20.56 ± 0.330 mV) values were chosen for experiments. The selected UA nanogels showed effective antimicrobial activity against and great wound healing properties. The results indicated that suitable UA nanogels with desired properties could be prepared. The therapeutic potential of the nanogels for oral ulcers was assessed using an animal model and the histopathological findings suggested that the optimized formulation is a good choice for oral ulcer treatment. Nonetheless, further research is recommended to support its efficacy by applying pharmacodynamic and pharmacokinetic studies in human individuals.

摘要

本研究旨在提供一种针对口腔溃疡的有效配方,使药物在应用部位停留更长时间,减少给药频率。作为候选配方,将乌那酸(UA)载入最佳纳米凝胶中。特性研究包括物理、流变学和生物黏附特性以及释放和透皮研究。流变学结果表明,纳米凝胶呈现假塑性流动行为。药物释放呈现延长的模式。此外,所选的 UA 纳米凝胶显示出非常低的穿透和渗透百分比。F13 显示出最高的释放率、适宜的生物黏附特性(0.475 ± 0.033 N/cm)和合适的粒径(250.22 ± 4.11 nm)、PDI(0.089 ± 0.052)和 Zeta 电位(20.56 ± 0.330 mV)值,被选为透皮实验。所选的 UA 纳米凝胶对金黄色葡萄球菌和白色念珠菌显示出有效的抗菌活性和良好的伤口愈合性能。结果表明,可以制备具有所需特性的合适 UA 纳米凝胶。通过动物模型评估纳米凝胶对口腔溃疡的治疗潜力,组织病理学发现表明,优化配方是治疗口腔溃疡的良好选择。然而,建议进行进一步的研究,通过在人体个体中应用药效学和药代动力学研究来支持其疗效。

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