Casula Luca, Lai Francesco, Pini Elena, Valenti Donatella, Sinico Chiara, Cardia Maria Cristina, Marceddu Salvatore, Ailuno Giorgia, Fadda Anna Maria
Dipartimento di Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, Università degli Studi di Cagliari, 09124 Cagliari, Italy.
DISFARM, Sezione di Chimica Generale e Organica "A. Marchesini", Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy.
Pharmaceutics. 2021 Aug 20;13(8):1300. doi: 10.3390/pharmaceutics13081300.
Curcumin has shown a potential extraordinary activity as an add-on ingredient in asthma treatment, due to its immunomodulatory and anti-inflammatory mechanism of action. However, its low water solubility and bioavailability lead to a poor therapeutic effect, which can be overcome by its formulation as nanocrystals. The aim of this study was to prepare a multicomponent formulation for the delivery of curcumin (CUR) and beclomethasone dipropionate (BDP) into the lungs as water-based nanosuspensions (NS). Single component formulations (CUR-NS, BDP-NS) and a multicomponent formulation (CUR+BDP-NS) were prepared through a wet ball media milling technique, using P188 as a non-toxic stabilizer. Characterization was carried out in terms of size, size distribution, zeta potential, nanocrystals morphology, and solid-state properties. Moreover, the inhalation delivery efficiency was studied with Next Generation Impactor (NGI, Apparatus E Ph. Eu). CUR-NS was optimized and showed a long-term stability and improved nanocrystals apparent solubility. The three formulations exhibited a nanocrystal mean diameter in the range of 200-240 nm and a homogenous particle size distribution. Aggregation or sedimentation phenomena were not observed in the multicomponent formulation on 90 days storage at room temperature. Finally, the nebulization tests of the three samples showed optimal aerodynamic parameters and MMAD < 5 µm.
姜黄素由于其免疫调节和抗炎作用机制,在哮喘治疗中作为一种附加成分显示出潜在的非凡活性。然而,其低水溶性和生物利用度导致治疗效果不佳,而将其制成纳米晶体可以克服这一问题。本研究的目的是制备一种多组分制剂,将姜黄素(CUR)和二丙酸倍氯米松(BDP)作为水基纳米混悬液(NS)递送至肺部。通过湿球介质研磨技术,使用P188作为无毒稳定剂,制备了单一组分制剂(CUR-NS、BDP-NS)和多组分制剂(CUR+BDP-NS)。从尺寸、尺寸分布、zeta电位、纳米晶体形态和固态性质方面进行了表征。此外,使用下一代撞击器(NGI,欧洲药典装置E)研究了吸入给药效率。CUR-NS经过优化,显示出长期稳定性并提高了纳米晶体的表观溶解度。这三种制剂的纳米晶体平均直径在200-240nm范围内,粒径分布均匀。在室温下储存90天时,多组分制剂中未观察到聚集或沉降现象。最后,这三个样品的雾化试验显示出最佳的空气动力学参数,且MMAD<5μm。
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