RESPONSE SURFACE METHODOLOGY-AIDED DEVELOPMENT OF PIRFENIDONE-LOADED SOLID LIPID NANOPARTICLES FOR INTRAPULMONARY DRUG DELIVERY SYSTEM

Kevin Kwok, G. Suhariyono, Silvia Surini
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Abstract

Objective: This study aims to determine the optimized Pirfenidone-loaded Solid Lipid Nanoparticles (P-SLN) formula for Intrapulmonary Drug Delivery System (IPDDS) using Response Surface Methodology (RSM). Methods: Box-Behnken design was applied to create fifteen P-SLN formulas comprising three independent variables, namely lipid-to-drug ratio, polymer type, and polymer concentration, and three dependent variables, including particle size, Polydispersity Index (PDI), and entrapment efficiency. The P-SLNs were prepared by solvent injection followed by the ultrasonication method. Those formulas were optimized with the RSM approach using the Design Expert®. Then, the optimized P-SLN was further characterized for morphology, moisture content, aerodynamic performance, and dissolution profile. Results: The optimization process, assisted by RSM, determined that the optimized P-SLN had a lipid-to-drug ratio of 6:1 and contained 0.5% Plasdone K-29/32. The resulting P-SLN had a spherical shape with a particle size of 212.7 nm, a PDI of 0.39, an entrapment efficiency of 95.02%, and a low moisture content of 1.59%. The optimized P-SLN also exhibited appropriate IPDDS required characteristics, including a Mass Median Aerodynamic Diameter (MMAD) ranging from 0.540–12.122 μm and a Respirable Fraction (RF) of 12.4%. Moreover, the release of pirfenidone from this optimized formula was 89.61% and 69.28% in pH 4.5 and 7.4 buffer media, respectively, in 45 min through a combination of diffusion and polymer swelling mechanisms. Conclusion: The optimized P-SLN showed promising potential as an IPDDS for pirfenidone.
响应面方法辅助开发用于肺内给药系统的吡非尼酮负载固体脂质纳米颗粒
研究目的本研究旨在利用响应面法(RSM)确定用于肺内给药系统(IPDDS)的优化吡非尼酮负载固体脂质纳米颗粒(P-SLN)配方:方法:采用盒-贝肯(Box-Behnken)设计创建了15种P-SLN配方,其中包括三个自变量(即脂药比、聚合物类型和聚合物浓度)和三个因变量(包括粒度、多分散指数(PDI)和包埋效率)。P-SLNs 采用溶剂注入法和超声法制备。利用 Design Expert® 的 RSM 方法对这些配方进行了优化。然后,进一步对优化后的 P-SLN 的形态、含水量、空气动力学性能和溶解曲线进行表征:结果:在 RSM 辅助下进行的优化过程确定,优化后的 P-SLN 的脂药比为 6:1,含 0.5% 的 Plasdone K-29/32。所得 P-SLN 呈球形,粒径为 212.7 纳米,PDI 为 0.39,包埋效率为 95.02%,水分含量低至 1.59%。优化后的 P-SLN 还具有 IPDDS 所需的适当特性,包括质量中值空气动力学直径(MMAD)范围为 0.540-12.122 μm,可吸入分数(RF)为 12.4%。此外,在 pH 值为 4.5 和 7.4 的缓冲介质中,通过扩散和聚合物溶胀相结合的机制,45 分钟内该优化配方中吡非尼酮的释放率分别为 89.61% 和 69.28%:结论:优化后的 P-SLN 显示出作为吡非尼酮 IPDDS 的巨大潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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