Respiratory Technology, Woolcock Institute of Medical Research and Discipline of Pharmacology, Faculty of Medicine and Health, The University of Sydney, 431 Glebe Point Road, Glebe, New South Wales 2037, Australia; Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technology (COSMAST), University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy.
Respiratory Technology, Woolcock Institute of Medical Research and Discipline of Pharmacology, Faculty of Medicine and Health, The University of Sydney, 431 Glebe Point Road, Glebe, New South Wales 2037, Australia.
J Pharm Sci. 2019 Sep;108(9):2964-2971. doi: 10.1016/j.xphs.2019.04.015. Epub 2019 Apr 19.
The pathogenesis and progression of several lung disorders is propagated by inflammatory and oxidative processes, which can be controlled by adjunctive inhaled therapies. The present study aimed to develop an inhalable dry powder formulation consisting of co-spray-dried urea-crosslinked hyaluronic acid and sodium ascorbyl phosphate (SD HA-CL-SAP), a novel combination which was recently shown to possess anti-inflammatory, antioxidant, and wound healing properties. Native HA and SAP were co-spray dried (SD HA-SAP) and evaluated as control formulation. Yield (Y%) and encapsulation efficiency (EE%) were 67.0 ± 4.8% and 75.5 ± 7.2% for SD HA-SAP, 70.0 ± 1.5% and 66.5 ± 5.7% for SD HA-CL-SAP, respectively. Both formulations were shown to be suitable for lung delivery in terms of morphology, particle size (median volumetric diameter ∼ 3.4 μm), physical and thermal stability, in vitro aerosol performance - respirable fraction: 30.5 ± 0.7% for SD HA-SAP and 35.3 ± 0.3% for SD HA-CL-SAP. SAP release was investigated using Franz cells and air-interface Calu-3 cell model (>90% of SAP transported within 4 h). The innovative SD HA-CL-SAP formulation holds potential as inhalable dry powder for the treatment of inflammatory lung disorders.
几种肺部疾病的发病机制和进展是由炎症和氧化过程传播的，可以通过辅助吸入疗法来控制。本研究旨在开发一种由喷雾共干燥的尿素交联透明质酸和抗坏血酸钠组成的可吸入干粉制剂（SD HA-CL-SAP），这是一种最近显示具有抗炎、抗氧化和伤口愈合特性的新型组合。天然 HA 和 SAP 进行了喷雾共干燥（SD HA-SAP），并作为对照制剂进行了评估。SD HA-SAP 的产率（Y%）和包封效率（EE%）分别为 67.0±4.8%和 75.5±7.2%，SD HA-CL-SAP 的产率（Y%）和包封效率（EE%）分别为 70.0±1.5%和 66.5±5.7%。这两种制剂在形态、粒径（中值体积直径约为 3.4μm）、物理和热稳定性、体外气溶胶性能方面都适合肺部给药-可吸入分数：SD HA-SAP 为 30.5±0.7%，SD HA-CL-SAP 为 35.3±0.3%。使用 Franz 细胞和空气界面 Calu-3 细胞模型研究了 SAP 的释放（>90%的 SAP 在 4h 内输送）。这种创新的 SD HA-CL-SAP 制剂具有作为治疗炎症性肺部疾病的可吸入干粉的潜力。
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