Saeed Muhammad Danish, Shah Kifayat Ullah, Nawaz Asif, Naz Faiqa Falak, Metouekel Amira, Shazly Gamal A, Dauelbait Musaab
Particle Design and Drug Delivery Laboratory, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, 29050, Khyber Pakhtunkhwa, Pakistan.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Universiti Malaya, Kuala Lumpur, 50603, Malaysia.
Sci Rep. 2025 Jul 1;15(1):20884. doi: 10.1038/s41598-025-05646-1.
To improve the solubility of atorvastatin and overcome the stability issues of liquid nanoemulsion, the current study aimed to synthesize solidified SNEDDS particles with aerodynamic diameter of ≤ 3 μm. The simple and chitosan-decorated liquid SNEDDS were dried by spray drying method and evaluated for their physicochemical properties, release characteristics and aerodynamic performance. A single dose pharmacokinetic study was performed in rabbits to establish the therapeutic performance of solidified nanoemulsion with respect to LIPITOR. The liquid SNEDDS were efficiently dried with pectin (1% w/w). The chitosan decorated solidified SNEDDS (SF10) have small particle size (2.02 μm), higher tapped density (0.733 g/cm) and smooth surface as compared to uncoated solidified SNEDDS (SF8). The chitosan coated SNEDDS had higher drug content and significantly lower roughness than uncoated SNEDDS (student t-test; p ≤ 0.01). The uncoated SNEDDS exhibited significantly higher burst drug release as compared to the chitosan coated SNEDDS due to the porous structure, amorphous nature and small size of its associated nanoemulsion. The solidified nanoemulsion had relatively lower MMAD (1.0 to 1.5 μm) that supports higher FPF values of 45-54% for the uncoated SNEDDS and chitosan coated SNEDDS, respectively. The pharmacokinetic study revealed that the solidified SNEDDS are superior with respect to its bioavailability being 1.5 times higher than LIPITOR.
为提高阿托伐他汀的溶解度并克服液体纳米乳剂的稳定性问题，本研究旨在合成空气动力学直径≤3μm的固化自乳化药物传递系统（SNEDDS）颗粒。通过喷雾干燥法对简单的、壳聚糖修饰的液体SNEDDS进行干燥，并对其理化性质、释放特性和空气动力学性能进行评估。在兔身上进行单剂量药代动力学研究，以确定固化纳米乳剂相对于立普妥的治疗性能。液体SNEDDS用果胶（1%w/w）有效干燥。与未包衣的固化SNEDDS（SF8）相比，壳聚糖修饰的固化SNEDDS（SF10）粒径小（2.02μm）、振实密度高（0.733g/cm）且表面光滑。壳聚糖包衣的SNEDDS药物含量更高，粗糙度明显低于未包衣的SNEDDS（学生t检验；p≤0.01）。由于其相关纳米乳剂的多孔结构、无定形性质和小尺寸，未包衣的SNEDDS与壳聚糖包衣的SNEDDS相比表现出显著更高的突释药物量。固化纳米乳剂的平均质量空气动力学直径（MMAD）相对较低（1.0至1.5μm），分别支持未包衣的SNEDDS和壳聚糖包衣的SNEDDS具有45-54%的较高肺部药物传递分数（FPF）值。药代动力学研究表明，固化的SNEDDS在生物利用度方面更优，比立普妥高1.5倍。
