使用初级、共轭和去共轭胆汁酸的纳米包封格列齐特的制剂浮力
Formulation buoyancy of nanoencapsulated gliclazide using primary, conjugated and deconjugated bile acids.
作者信息
Mathavan Sangeetha, Ionescu Corina M, Kovacevic Bozica, Mikov Momir, Golocorbin-Kon Svetlana, Mooranian Armin, Dass Crispin R, Al-Salami Hani
机构信息
Biotechnology & Drug Development Research Laboratory, School of Pharmacy & Biomedical Science, Curtin Health Innovation Research Institute, Curtin University, Kent Street, Bentley 6102, Perth, WA, Australia.
Molecular Biology & Biotechnology Department, Faculty of Biology & Geology, Babes-Bolyai University, 5-7 Clinicilor St, Cluj-Napoca 400006, Romania.
出版信息
Ther Deliv. 2019 Sep;10(9):573-583. doi: 10.4155/tde-2019-0058. Epub 2019 Oct 24.
Recent studies suggest potential applications of endogenously produced human bile acids as formulation-excipient and drug tissue permeation enhancers in Type 1 diabetes. We aimed to examine the stability, tissue permeation and muscle-cell effects of microencapsulated gliclazide (G) incorporated with a primary (chenodeoxycholic acid [CDCA]), a secondary (ursodeoxycholic acid [UDCA]) or a tertiary (taurocholic acid [TCA]) bile acid. Four formulations made of sodium alginate, CDCA, UDCA and TCA were examined for buoyancy, tissue-enhancing effects () and local () viability effects. CDCA, UDCA and TCA improved buoyancy and cell viability but not tissue-specific uptake. G-TCA-sodium alginate microcapsules exerted hypoglycemic effects, suggesting significant improvement of G gut-uptake by TCA, possibly via improving buoyancy.
近期研究表明，内源性产生的人胆汁酸在1型糖尿病中作为制剂辅料和药物组织渗透促进剂具有潜在应用价值。我们旨在研究微囊化格列齐特（G）与初级胆汁酸（鹅去氧胆酸[CDCA]）、次级胆汁酸（熊去氧胆酸[UDCA]）或三级胆汁酸（牛磺胆酸[TCA]）结合后的稳定性、组织渗透性和对肌肉细胞的影响。对由海藻酸钠、CDCA、UDCA和TCA制成的四种制剂进行了浮力、组织增强作用（）和局部（）活力影响的检测。CDCA、UDCA和TCA提高了浮力和细胞活力，但未提高组织特异性摄取。G-TCA-海藻酸钠微囊具有降血糖作用，表明TCA可能通过改善浮力显著提高了G的肠道摄取。
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