Laboratory of Investigation in Chronic Diseases, Department of Physiological Sciences, Center of Biological Sciences, Federal University of Santa Catarina, Florianópolis, Brazil.
Graduate Program in Pharmacology, Center of Biological Sciences, Federal University of Santa Catarina, Florianópolis, Brazil.
Drug Deliv Transl Res. 2023 Nov;13(11):2948-2959. doi: 10.1007/s13346-023-01367-y. Epub 2023 May 19.
Mometasone furoate (MF) is a synthetic glucocorticoid used clinically to treat specific inflammatory disorders including superior and inferior respiratory tract. Due to its poor bioavailability we further investigated whether nanoparticles (NPs) made of zein protein may constitute a safe and effective choice to incorporate MF. Thus, in this work, we loaded MF into zein NPs aiming to evaluate possible advantages that could result from oral delivery and extend the range of MF application such as inflammatory gut diseases. MF-loaded zein NPs presented an average size in the range of 100 and 135 nm, narrow size distribution (polydispersity index < 0.300), zeta potential of around + 10 mV and association efficiency of MF over 70%. Transmission electron microscopy imaging revealed that NPs had a round shape and presented a smooth surface. The zein NPs showed low MF release in a buffer that mimics the gastric condition (pH = 1.2) and slower and controlled MF release in the intestinal condition (pH = 6.8). The short and intermediate safety of zein NPs was confirmed assessing the incubation against Caco-2 and HT29-MTX intestinal cells up to 24 h. Permeability studies of MF across Caco-2/HT29-MTX co-culture monolayer evidenced that zein NPs modulated MF transport across cell monolayer resulting in a stronger and prolonged interaction with mucus, potentially extending the time of absorption and overall local and systemic bioavailability. Overall, zein NPs showed to be suitable to carry MF to the intestine and future studies can be developed to investigate the use of MF-loaded zein NPs to treat intestinal inflammatory diseases.
糠酸莫米松（MF）是一种合成的糖皮质激素，临床上用于治疗特定的炎症性疾病，包括上呼吸道和下呼吸道。由于其生物利用度差，我们进一步研究了玉米醇溶蛋白制成的纳米颗粒（NPs）是否可以作为一种安全有效的选择来包裹 MF。因此，在这项工作中，我们将 MF 负载到玉米醇溶蛋白 NPs 中，旨在评估口服给药可能带来的优势，并扩展 MF 的应用范围，如炎症性肠道疾病。载 MF 的玉米醇溶蛋白 NPs 的平均粒径在 100-135nm 范围内，粒径分布较窄（多分散指数<0.300），zeta 电位约为+10mV，MF 的结合效率超过 70%。透射电子显微镜成像显示 NPs 呈圆形且表面光滑。玉米醇溶蛋白 NPs 在模拟胃条件（pH=1.2）的缓冲液中表现出低 MF 释放，而在肠条件（pH=6.8）中则表现出缓慢和受控的 MF 释放。通过评估对 Caco-2 和 HT29-MTX 肠细胞的孵育至 24 小时，证实了玉米醇溶蛋白 NPs 的短期和中期安全性。MF 通过 Caco-2/HT29-MTX 共培养单层的渗透性研究表明，玉米醇溶蛋白 NPs 调节 MF 在细胞单层中的转运，导致与粘液的相互作用更强、更持久，可能延长吸收时间和整体局部和全身生物利用度。总的来说，玉米醇溶蛋白 NPs 适合将 MF 递送到肠道，未来的研究可以开发 MF 负载的玉米醇溶蛋白 NPs 用于治疗肠道炎症性疾病。
