Corrugated surface microparticles with chitosan and levofloxacin for improved aerodynamic performance

IF 10.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Asian Journal of Pharmaceutical Sciences Pub Date : 2023-05-01 DOI:10.1016/j.ajps.2023.100815
Chang-Soo Han , Ji-Hyun Kang , Eun hye Park , Hyo-Jung Lee , So-Jeong Jeong , Dong-Wook Kim , Chun-Woong Park
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Abstract

Corrugated surface microparticles comprising levofloxacin (LEV), chitosan and organic acid were prepared using the 3-combo spray drying method. The amount and the boiling point of the organic acid affected the degree of roughness. In this study, we tried to improve the aerodynamic performance and increase aerosolization by corrugated surface microparticle for lung drug delivery efficiency as dry powder inhaler. HMP175 L20 prepared with 175 mmol propionic acid solution was corrugated more than HMF175 L20 prepared with 175 mmol formic acid solution. The ACI and PIV results showed a significant increase in aerodynamic performance of corrugated microparticles. The FPF value of HMP175 L20 was 41.3% ± 3.9% compared with 25.6% ± 7.7% of HMF175 L20. Corrugated microparticles also showed better aerosolization, decreased x-axial velocity, and variable angle. Rapid dissolution of drug formulations was observed in vivo. Low doses administered to the lungs achieved higher LEV concentrations in the lung fluid than high doses administered orally. Surface modification in the polymer-based formulation was achieved by controlling the evaporation rate and improving the inhalation efficiency of DPIs.

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壳聚糖和左氧氟沙星用于改善空气动力学性能的波纹表面微粒
采用三元喷雾干燥法制备了含有左氧氟沙星、壳聚糖和有机酸的波纹表面微粒。有机酸的量和沸点影响粗糙度。在本研究中,我们试图通过波纹表面微粒改善空气动力学性能,并增加雾化作用,以提高干粉吸入器的肺部药物输送效率。用175毫摩尔丙酸溶液制备的HMP175 L20比用175毫毫摩尔甲酸溶液制得的HMF175 L20波纹更大。ACI和PIV结果显示波纹微粒的空气动力学性能显著提高。HMP175 L20的FPF值为41.3%±3.9%,而HMF175 L20为25.6%±7.7%。波纹状微粒也表现出更好的雾化、降低的x轴速度和可变角度。在体内观察到药物制剂的快速溶解。给予肺部的低剂量比口服给予的高剂量在肺液中获得更高的LEV浓度。聚合物基制剂的表面改性是通过控制DPI的蒸发速率和提高吸入效率来实现的。
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来源期刊
Asian Journal of Pharmaceutical Sciences
Asian Journal of Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
18.30
自引率
2.90%
发文量
11
审稿时长
14 days
期刊介绍: The Asian Journal of Pharmaceutical Sciences (AJPS) serves as the official journal of the Asian Federation for Pharmaceutical Sciences (AFPS). Recognized by the Science Citation Index Expanded (SCIE), AJPS offers a platform for the reporting of advancements, production methodologies, technologies, initiatives, and the practical application of scientific knowledge in the field of pharmaceutics. The journal covers a wide range of topics including but not limited to controlled drug release systems, drug targeting, physical pharmacy, pharmacodynamics, pharmacokinetics, pharmacogenomics, biopharmaceutics, drug and prodrug design, pharmaceutical analysis, drug stability, quality control, pharmaceutical engineering, and material sciences.
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