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载有生物活性芹菜素的口服纳米双分子层脂质体：从制剂优化到临床前评估

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment.

作者信息

Zafar Ameeduzzafar, Alruwaili Nabil K, Imam Syed Sarim, Hadal Alotaibi Nasser, Alharbi Khalid Saad, Afzal Muhammad, Ali Raisuddin, Alshehri Sultan, Alzarea Sami I, Elmowafy Mohammed, Alhakamy Nabil A, Ibrahim Mohamed F

机构信息

Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Aljouf 72341, Saudi Arabia.

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

出版信息

Saudi Pharm J. 2021 Mar;29(3):269-279. doi: 10.1016/j.jsps.2021.02.003. Epub 2021 Feb 22.

DOI:10.1016/j.jsps.2021.02.003
PMID:33981176
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8085606/
Abstract

AIM

Diabetic (type-2) is a metabolic disease characterized by increased blood glucose level from the normal level. In the present study, apigenin (AG) loaded lipid vesicles (bilosomes: BIL) was prepared, optimized and evaluated for the oral therapeutic efficacy.

EXPERIMENTAL

AG-BIL was prepared by a thin-film evaporation method using cholesterol, span 60 and sodium deoxycholate. The prepared formulation was optimized by 3-factor and 3-level Box-Behnken design using particle size, entrapment efficiency and drug release as a response. The selected formulation further evaluated for  permeation,  pharmacokinetic and pharmacodynamics study.

RESULTS

The optimized AG bilosomes (AG-BILopt) has shown the vesicle size 183.25 ± 2.43 nm, entrapment efficiency 81.67 ± 4.87%. TEM image showed a spherical shape vesicle with sharp boundaries. The drug release study revealed a significant enhancement in AG release (79.45 ± 4.18%) from AG-BILopt as compared to free AG-dispersion (25.47 ± 3.64%). The permeation and pharmacokinetic studies result revealed 4.49 times higher flux and 4.67 folds higher AUC than free AG-dispersion. The antidiabetic activity results showed significant (P < 0.05) enhancement in therapeutic efficacy than free AG-dispersion. The results also showed marked improvement in biochemical parameters.

CONCLUSION

Our findings suggested, the prepared apigenin loaded bilosomes was found to be an efficient delivery in the therapeutic efficacy in diabetes.

摘要

目的

2型糖尿病是一种代谢性疾病，其特征是血糖水平高于正常水平。在本研究中，制备了载有芹菜素（AG）的脂质囊泡（双分子层脂质体：BIL），对其进行优化并评估口服治疗效果。

实验

采用胆固醇、司盘60和脱氧胆酸钠，通过薄膜蒸发法制备AG-BIL。使用粒径、包封率和药物释放作为响应变量，通过三因素三水平的Box-Behnken设计对制备的制剂进行优化。对所选制剂进一步进行渗透、药代动力学和药效学研究。

结果

优化后的AG双分子层脂质体（AG-BILopt）的囊泡大小为183.25±2.43nm，包封率为81.67±4.87%。透射电镜图像显示为边界清晰的球形囊泡。药物释放研究表明，与游离AG分散体（25.47±3.64%）相比，AG-BILopt的AG释放显著增强（79.45±4.18%）。渗透和药代动力学研究结果显示，通量比游离AG分散体高4.49倍，AUC高4.67倍。抗糖尿病活性结果显示，治疗效果比游离AG分散体显著增强（P<0.05）。结果还显示生化参数有明显改善。

结论

我们的研究结果表明，制备的载芹菜素双分子层脂质体在糖尿病治疗中是一种有效的给药方式。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/ec6fede65c40/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/fbb61c2d84cb/gr1a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/68d4016a68ea/gr1b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/f4ceab95edf7/gr1c.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/7025ab85fca6/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/52daec34f965/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/4d22e1a36dae/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/02226816d26d/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/3887192f8a0c/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/ec6fede65c40/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/fbb61c2d84cb/gr1a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/68d4016a68ea/gr1b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/f4ceab95edf7/gr1c.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/7025ab85fca6/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/52daec34f965/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/4d22e1a36dae/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/02226816d26d/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/3887192f8a0c/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c078/8085606/ec6fede65c40/gr7.jpg

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J Pharm Pharmacol. 2020 Nov;72(11):1645-1656. doi: 10.1111/jphp.13347. Epub 2020 Aug 2.
2
Bile acid transporter-mediated oral drug delivery.胆汁酸转运体介导的口服药物递送。
J Control Release. 2020 Nov 10;327:100-116. doi: 10.1016/j.jconrel.2020.07.034. Epub 2020 Jul 22.
3
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4
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Ther Deliv. 2025 May;16(5):487-500. doi: 10.1080/20415990.2025.2469488. Epub 2025 Mar 24.
5
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6
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7
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