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Design and evaluation of inhalable nanocrystals embedded microparticles with enhanced redispersibility and bioavailability for breviscapine
Powder Technology ( IF 5.2 ) Pub Date : 2021-01-01 , DOI: 10.1016/j.powtec.2020.08.040
Yingchong Chen , Yan Gui , Yijing Luo , Yang Liu , Liangxing Tu , Yueqin Ma , Pengfei Yue , Ming Yang

The purpose of this study was to design novel inhalable nanocrystals embedded microparticles for pulmonary delivery of breviscapine (BVC). The TPGS modified BVC nanocrystals (BVC-NC@TPGS) were fabricated by high pressure homogenization. And the BVC-NC@TPGS was further converted into nanocrystals-embedded microparticles (BVC-NEP) via spray-drying. The influence of matrix formers and concentration on the properties of BVC-NEP for inhalation was investigated. The particle size, morphology, drug crystal state, in vitro aerodynamic performance, in vitro release behavior and pharmacokinetic behaviors were characterized. It was demonstrated that the morphology, lung deposition as well as in vitro drug release from the microparticles were significantly influenced by matrix formers type and concentration. BVC-NEP with 10% TPGS as stabilizer and 200% MN as matrix formers presented the highest FPF value and most excellent flowability as well as redispersibility. Further the in vivo pharmacokinetic studies demonstrated that the AUC₍₀₋∞₎ of the inhalable BVC-NEP/MN (1411.099 ± 334.62 μg/L h) was 6.29 times (p < 0.05) as high as that of the coarse BVC (224.21 ± 59.47 μg/L h), and not significantly from that of BVC injection. Therefore, inhalable nanocrystals-embedded microparticles could be a promising strategy for pulmonary delivery of poorly soluble drugs that was unfittable for oral administration.

中文翻译:

可吸入纳米晶体嵌入微粒的设计和评估具有增强的灯盏花素再分散性和生物利用度

本研究的目的是设计新型可吸入纳米晶体嵌入微粒,用于灯盏花素 (BVC) 的肺部递送。TPGS 改性的 BVC 纳米晶体(BVC-NC@TPGS)是通过高压均质化制备的。通过喷雾干燥将 BVC-NC@TPGS 进一步转化为纳米晶体嵌入的微粒(BVC-NEP)。研究了基质形成剂和浓度对 BVC-NEP 吸入特性的影响。表征了粒径、形态、药物晶态、体外空气动力学性能、体外释放行为和药代动力学行为。结果表明,微颗粒的形态、肺沉积以及体外药物释放受基质形成剂类型和浓度的显着影响。含有 10% TPGS 作为稳定剂和 200% MN 作为基质形成剂的 BVC-NEP 表现出最高的 FPF 值和最优异的流动性以及再分散性。此外,体内药代动力学研究表明,可吸入 BVC-NEP/MN (1411.099 ± 334.62 μg/L h) 的 AUC₍₀₋∞₎ 是粗 BVC (224.21) 的 6.29 倍 (p < 0.05) ± 59.47 μg/L h),与 BVC 注射相比没有显着差异。因此,可吸入纳米晶体嵌入的微粒可能是一种有前途的策略,可用于肺部递送不适合口服的难溶性药物。是粗 BVC (224.21 ± 59.47 μg/L h) 的 29 倍 (p < 0.05),与 BVC 注射相比没有显着差异。因此,可吸入纳米晶体嵌入的微粒可能是一种有前途的策略,可用于肺部递送不适合口服的难溶性药物。是粗 BVC (224.21 ± 59.47 μg/L h) 的 29 倍 (p < 0.05),与 BVC 注射相比没有显着差异。因此,可吸入纳米晶体嵌入的微粒可能是一种有前途的策略,可用于肺部递送不适合口服的难溶性药物。
更新日期:2021-01-01
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