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Proniosomal Microcarriers: Impact of Constituents on the Physicochemical Properties of Proniosomes as a New Approach to Enhance Inhalation Efficiency of Dry Powder Inhalers.
AAPS PharmSciTech ( IF 3.3 ) Pub Date : 2020-05-24 , DOI: 10.1208/s12249-020-01705-0
Amr Gamal 1 , Haitham Saeed 2 , Ossama M Sayed 1 , Rasha M Kharshoum 1 , Heba F Salem 1
Affiliation  

Proniosomes are free-flowing systems with coating carriers, which developed as a method for improving the drug flow and pulmonary delivery. Extensive research on proniosomes was done to enhance the dry powder inhalers (DPI)'s inhalation performance. This research aimed at studying the impact of lactose-mannitol mixture additives on the proniosome's physicochemical properties as a method for improving the inhalation efficiency of DPI. Vismodegib has been employed as a compound model. Box-Behnken design has been employed to prepare different proniosomes formulae by incorporating various (A) span 60 concentrations, (B) lactose concentrations and (C) mannitol: total carrier mixture. The measured responses were vesicle size (R1), %release (R2), Carr's index (R3) and %recovery (R4). The results displayed that R1 and R4 were significantly antagonistic to C and significantly synergistic to both A and B while R2 and R3 were significantly synergistic to C and significantly antagonistic to both A and B. The optimal formula was selected for its aerodynamic behaviour, cytotoxic activity and bioavailability assessment. The optimal formula resulted in better Vismodegib lung deposition, cytotoxic activity and relative bioavailability. This novel formula could be a promising carrier for sustained delivery of drugs via the pulmonary route.

中文翻译:

前体微载体:成分对前体的理化性质的影响,作为提高干粉吸入器吸入效率的新方法。

proniosomes是带有包衣载体的自由流动系统,已开发为改善药物流动和肺部递送的方法。为了增强干粉吸入器(DPI)的吸入性能,对前体小体进行了广泛的研究。这项研究旨在研究乳糖-甘露醇混合物添加剂对前体的理化性质的影响,作为提高DPI吸入效率的方法。Vismodegib已被用作复合模型。通过掺入各种(A)跨度60浓度,(B)乳糖浓度和(C)甘露醇:总载体混合物,采用Box-Behnken设计来制备不同的proniosome配方。测得的反应是囊泡大小(R1),释放%(R2),卡尔指数(R3)和恢复%(R4)。结果表明,R1和R4对C具有明显的拮抗作用,并且与A和B都具有明显的协同作用,而R2和R3与C具有明显的协同作用,并且对A和B具有明显的拮抗作用。和生物利用度评估。最佳配方可产生更好的Vismodegib肺沉积,细胞毒性活性和相对生物利用度。该新配方可能是通过肺途径持续递送药物的有希望的载体。最佳配方可导致更好的Vismodegib肺沉积,细胞毒性活性和相对生物利用度。该新配方可能是通过肺途径持续递送药物的有希望的载体。最佳配方可产生更好的Vismodegib肺沉积,细胞毒性活性和相对生物利用度。这种新颖的配方可能是通过肺途径持续递送药物的有希望的载体。
更新日期:2020-05-24
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