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罗勒新型微囊制剂对血糖和血脂谱的药理作用:一项临床前研究。

Pharmacological effects of novel microvesicles of basil, on blood glucose and the lipid profile: a preclinical study.

机构信息

Department of Pharmacy, Faculty of Medicine, University of Novi Sad, Hajduk Veljkova 3, 21000, Novi Sad, Serbia.

Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad, Hajduk Veljkova 3, Novi Sad, Serbia.

出版信息

Sci Rep. 2021 Nov 11;11(1):22123. doi: 10.1038/s41598-021-01713-5.

DOI:10.1038/s41598-021-01713-5
PMID:34764416
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8586354/
Abstract

Microencapsulation represents a process that can create targeted, controlled release kinetics of drugs, thus optimizing therapeutic efficacy. Our group has investigated the impact of this technology on Wistar rats to determine pharmacological efficacy of basil extracts. Animals were treated with water extract of Ocimum basilicum in microvesicles and with combination of basil extracts and 3α,7α-dihydroxy-12-keto-5-cholanate, also known as 12-monoketocholic acid (MKC) acid in microvesicles for 7 days. Alloxan was used to induce hyperglycemia. Pharmacological effects on glycemia were evaluated by measuring blood glucose levels in alloxan-induced diabetic rats. Microvesicles were prepared using the Büchi-based microencapsulating system developed in our lab. The dose of basil extract that was orally administered in rats was 200 mg/kg and the dose of MKC acid was 4 mg/kg as per established protocols. A seven-day treatment with basil aqueous extract, as well as a combination of basil and MKC acid extract in the pharmaceutical formulation, led to a statistically significant reduction in the blood glucose concentration of animals with alloxan-induced hyperglycemia compared to pre-treatment values (p < 0.05 and p < 0.01), which indicates that basil has hypoglycemic and antihyperglycemic effects. Microvesicles, as a pharmaceutical-technological formulation, substantially enhance the hypolipidemic action of basil extract with MKC acid.

摘要

微胶囊化是一种可以创造靶向、控制药物释放动力学的过程,从而优化治疗效果。我们的团队研究了这项技术对 Wistar 大鼠的影响,以确定罗勒提取物的药理学功效。动物用微囊中的罗勒水提取物和罗勒提取物与 3α,7α-二羟基-12-酮-5-胆酸(也称为 12-单酮胆酸,MKC 酸)的混合物处理 7 天。用链脲佐菌素诱导高血糖。通过测量链脲佐菌素诱导的糖尿病大鼠的血糖水平来评估对血糖的药理作用。微囊使用我们实验室开发的基于 Büchi 的微囊化系统制备。按照既定方案,大鼠口服罗勒提取物的剂量为 200mg/kg,MKC 酸的剂量为 4mg/kg。用罗勒水提取物以及罗勒和 MKC 酸提取物的组合进行为期 7 天的治疗,与治疗前相比,可显著降低链脲佐菌素诱导的高血糖动物的血糖浓度(p<0.05 和 p<0.01),这表明罗勒具有降血糖和抗高血糖作用。微囊作为一种药物技术制剂,大大增强了含有 MKC 酸的罗勒提取物的降血脂作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/228d/8586354/1713025bbcbb/41598_2021_1713_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/228d/8586354/ef84cb4fbede/41598_2021_1713_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/228d/8586354/1713025bbcbb/41598_2021_1713_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/228d/8586354/ef84cb4fbede/41598_2021_1713_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/228d/8586354/1713025bbcbb/41598_2021_1713_Fig2_HTML.jpg

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本文引用的文献

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Plant Foods Hum Nutr. 2021 Jun;76(2):240-247. doi: 10.1007/s11130-021-00902-x. Epub 2021 Jun 9.
2
High-Loading Dose of Microencapsulated Gliclazide Formulation Exerted a Hypoglycaemic Effect on Type 1 Diabetic Rats and Incorporation of a Primary Deconjugated Bile Acid, Diminished the Hypoglycaemic Antidiabetic Effect.高负荷剂量的微囊化格列齐特制剂对1型糖尿病大鼠具有降血糖作用,而加入一种初级去共轭胆汁酸会减弱这种降血糖抗糖尿病作用。
Eur J Drug Metab Pharmacokinet. 2017 Dec;42(6):1005-1011. doi: 10.1007/s13318-017-0415-0.
3
The Influence of Stabilized Deconjugated Ursodeoxycholic Acid on Polymer-Hydrogel System of Transplantable NIT-1 Cells.稳定去共轭熊去氧胆酸对可移植NIT-1细胞聚合物水凝胶系统的影响
Pharm Res. 2016 May;33(5):1182-90. doi: 10.1007/s11095-016-1863-y. Epub 2016 Jan 27.
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Swelling, mechanical strength, and release properties of probucol microcapsules with and without a bile acid, and their potential oral delivery in diabetes.载有和未载有胆酸的普罗布考微囊的肿胀度、机械强度和释放性能及其在糖尿病中的口服递送潜力。
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An optimized probucol microencapsulated formulation integrating a secondary bile acid (deoxycholic acid) as a permeation enhancer.一种优化的普罗布考微囊化制剂,其整合了一种次级胆汁酸(脱氧胆酸)作为渗透促进剂。
Drug Des Devel Ther. 2014 Sep 29;8:1673-83. doi: 10.2147/DDDT.S68247. eCollection 2014.
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