Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad, Pakistan.
Ocular Therapeutics Research Group, Pharmaceutical and Molecular Biotechnology Research Centre, Department of Science, Waterford Campus, South East Technological University (SETU), Waterford, Ireland.
Expert Opin Drug Deliv. 2024 May;21(5):779-796. doi: 10.1080/17425247.2024.2361117. Epub 2024 May 31.
Controlled and targeted drug delivery to treat nonalcoholic fatty liver disease (NAFLD) can benefit from additive attributes of natural formulation ingredients incorporated into the drug delivery vehicles.
Lovastatin (LVN) loaded, bile acid (BA) and fatty acid (FA) integrated nanoemulsomes (NES) were formulated by thin layer hydration technique for synergistic and targeted delivery of LVN to treat NAFLD. Organic phase NES was comprised of stearic acid with garlic (GL) and ginger (GR) oils, separately. Ursodeoxycholic acid and linoleic acid were individually incorporated as targeting moieties.
Stability studies over 90 days showed average NES particle size, surface charge, polydispersity index, and entrapment efficiency values of 270 ± 27.4 nm, -23.8 ± 3.5 mV, 0.2 ± 0.04 and 81.36 ± 3.4%, respectively. Spherical NES were observed under a transmission electron microscope. LVN release depicted non-fickian release mechanisms from GL and GR oils-based NES. permeation of BA/FA integrated NES through isolated rat intestines showed greater flux than non-integrated ones.
Liver histopathology of experimental rats together with in-vivo lipid profiles and liver function tests illustrated that these NES possess the clinical potential to be promising drug carriers for NAFLD.
控制和靶向药物输送治疗非酒精性脂肪性肝病（NAFLD）可以受益于天然配方成分的附加属性，这些属性被整合到药物输送载体中。
通过薄层水化技术制备载洛伐他汀（LVN）、胆酸（BA）和脂肪酸（FA）整合的纳米乳囊（NES），以协同和靶向输送 LVN 来治疗 NAFLD。有机相 NES 由硬脂酸与大蒜（GL）和姜（GR）油组成，分别。熊去氧胆酸和亚油酸分别作为靶向部分被整合。
90 天的稳定性研究显示，平均 NES 粒径、表面电荷、多分散指数和包封效率值分别为 270±27.4nm、-23.8±3.5mV、0.2±0.04 和 81.36±3.4%。在透射电子显微镜下观察到球形 NES。GL 和 GR 油基 NES 中的 LVN 释放呈现非菲克扩散机制。BA/FA 整合的 NES 通过分离的大鼠肠的渗透显示出比非整合的 NES 更高的通量。
实验大鼠的肝脏组织病理学以及体内脂质谱和肝功能测试表明，这些 NES 具有成为治疗 NAFLD 的有前途的药物载体的临床潜力。
