首页> 外文期刊>Drug development and industrial pharmacy >Inhalable liposomes of Glycyrrhiza glabra extract for use in tuberculosis: formulation, in vitro characterization, in vivo lung deposition, and in vivo pharmacodynamic studies
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Inhalable liposomes of Glycyrrhiza glabra extract for use in tuberculosis: formulation, in vitro characterization, in vivo lung deposition, and in vivo pharmacodynamic studies

机译:Glycyrrhiza Glabra提取物用于结核病的可吸入式脂质体:制剂,体外表征,体内肺部沉积,体内药效学研究

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Objective: The current study involves the development of liposomal dry powder for inhalation (LDPI) containing licorice extract (LE) for use in tuberculosis. Significance: The current epidemiology of tuberculosis along with the increasing emergence of resistant forms of tuberculosis necessitates the need for developing alternative efficacious medicines for treatment, Licorice is a medicinal herb with reported activity against Mycobacterium tuberculosis. Methods: Liposomes with LE were prepared by thin film hydration technique and freeze dried to obtain LDPI. The comprehensive in vitro and in vivo characterization of the LDPI formulation was carried out. Results: The particle size of liposomes was around 210nm with drug entrapment of almost 75%. Transmission electron microscopy revealed spherical shape of liposome vesicles. The flow properties of the LDPI were within acceptable limits. Anderson Cascade Impactor studies showed the mean median aerodynamic diameter, geometric standard deviation and fine particle fraction of the LDPI to be 4.29 |im, 1.23, and 54.68%, respectively. In vivo lung deposition studies of LDPI in mice showed that almost 46% of the drug administered reaches the lungs and 16% of administered drug is retained in the lungs after 24 hours of administration. The in vivo pharmacodynamic evaluation of the LDPI showed significant reduction in bacterial counts in lungs as well as spleen of TB-infected mice. Conclusions: LE LDPI thus has a promising potential to be explored as an effective anti-tubercular medicine or as an adjunct to existing anti-tubercular drugs.
机译:目的:目前的研究涉及含有甘草提取物(LDPI)的脂质体干粉(LDPI)的开发,用于结核病。意义:结核病目前的流行病学随着抗性形式的耐药形式的越来越需要需要开发替代治疗的替代药物,甘草是一种药用草药,其报告的结核分枝杆菌的活性。方法:用薄膜水合作合金技术制备脂质体,并冷冻干燥,得到LDPI。进行了综合体外和体内表征的LDPI制剂。结果:脂质体的粒度约为210nm,药物夹杂物差约为75%。透射电子显微镜显示脂质体囊泡的球形形状。 LDPI的流量属性是可接受的限制。安德森级联影响力研究表明,LDPI的平均值空气动力直径,几何标准偏差和细粒分别分别为4.29,1.23和54.68%。在小鼠中的LDPI体内肺部沉积研究表明,近46%的药物施用到肺部达到肺部,并且在24小时后,在肺中保留16%的给药药物。 LDPI的体内药效学评估显示肺部细菌计数的显着降低以及TB感染的小鼠的脾脏。结论:LE LDPI因此有希望探索为有效的抗结核药物或作为现有抗结核药物的辅助潜力。

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