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柚皮素自微乳给药系统(SNEDDS)的溶解和抗氧化潜力及其口服给药。

Dissolution and antioxidant potential of apigenin self nanoemulsifying drug delivery system (SNEDDS) for oral delivery.

机构信息

Department of Pharmacy, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayuthaya Road, Rajathevi, Bangkok, 10400, Thailand.

Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok, 10400, Thailand.

出版信息

Sci Rep. 2024 Apr 17;14(1):8851. doi: 10.1038/s41598-024-59617-z.


DOI:10.1038/s41598-024-59617-z
PMID:38632321
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11024192/
Abstract

Self-nanoemulsifying drug delivery systems (SNEDDS) have been used to improve the oral bioavailability of various drugs. In the current study, apigenin was developed as SNEDDS to solve its dissolution problem and enhance oral bioavailability and antioxidant potential. SNEDDS were prepared by mixing Gelucire 44/14, Tween 80, and PEG 400 under controlled conditions. The droplet of diluted SNEDDS demonstrated a spherical shape with a size of less than 100 nm and a neutral charge. The very fast self-emulsification was obtained within 32 s, and the transmittance values exceeded 99%. The highest drug loading was 90.10 ± 0.24% of the initial load with the highest %encapsulation efficiency of 84.20 ± 0.03%. FT-IR and DSC spectra showed no interaction between components. The dissolution in buffer pH 1.2, 4.5, and 6.8 showed significantly higher dissolved apigenin than the apigenin coarse powder. The dissolution profiles were fitted to the Korsmeyer-Peppas kinetics. The cellular antioxidant activities in Caco-2 cells were approximately 52.25-54.64% compared to no treatment and were higher than the apigenin coarse powder (12.70%). Our work highlights the potential of SNEDDS to enhance the dissolution and permeability of apigenin and promote antioxidant efficacy, which has a strong chance of being developed as a bioactive compound for nutraceuticals.

摘要

自微乳药物传递系统(SNEDDS)已被用于改善各种药物的口服生物利用度。在本研究中,开发了芹菜素 SNEDDS 来解决其溶解问题并提高口服生物利用度和抗氧化潜力。SNEDDS 通过在控制条件下混合 Gelucire 44/14、吐温 80 和 PEG 400 来制备。稀释 SNEDDS 的液滴呈球形,尺寸小于 100nm,带中性电荷。非常快的自乳化在 32s 内完成,透光率值超过 99%。最高药物载量为初始载药量的 90.10±0.24%,最高包封效率为 84.20±0.03%。FT-IR 和 DSC 图谱显示成分之间没有相互作用。在缓冲液 pH 值 1.2、4.5 和 6.8 中的溶解度显示出比芹菜素粗粉明显更高的溶解芹菜素。溶解曲线拟合到 Korsmeyer-Peppas 动力学。Caco-2 细胞中的细胞抗氧化活性与无处理相比约为 52.25-54.64%,高于芹菜素粗粉(12.70%)。我们的工作强调了 SNEDDS 提高芹菜素溶解度和通透性并促进抗氧化功效的潜力,这使其很有机会被开发为用于营养保健品的生物活性化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/f437947ff152/41598_2024_59617_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/f9fcde252dd5/41598_2024_59617_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/98743bd54b3c/41598_2024_59617_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/d768ef35f90f/41598_2024_59617_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/33312d8b0069/41598_2024_59617_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/f437947ff152/41598_2024_59617_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/f9fcde252dd5/41598_2024_59617_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/98743bd54b3c/41598_2024_59617_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/d768ef35f90f/41598_2024_59617_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/33312d8b0069/41598_2024_59617_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38c7/11024192/f437947ff152/41598_2024_59617_Fig5_HTML.jpg

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引用本文的文献

[1]
The Protective Activity of Apigenin Against Bone and Cartilage Diseases.

Clin Interv Aging. 2025-8-13

[2]
Targeting drug resistant colorectal cancer with apigenin nanoarchitectures.

Transl Oncol. 2025-6-24

[3]
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Int J Mol Sci. 2025-5-8

[4]
Pharmacogenomics influence on MDR1-associated cancer resistance and innovative drug delivery approaches: advancing precision oncology.

Med Oncol. 2025-2-6

[5]
Enhancement of in vitro transcellular absorption and in vivo oral bioavailability of apigenin by self-nanoemulsifying drug delivery systems.

Sci Rep. 2024-12-30

本文引用的文献

[1]
Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Apremilast: In Vitro Evaluation and Pharmacokinetics Studies.

Molecules. 2022-5-11

[2]
Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS).

Pharmaceutics. 2022-2-22

[3]
Current Status and Future Perspectives on Therapeutic Potential of Apigenin: Focus on Metabolic-Syndrome-Dependent Organ Dysfunction.

Antioxidants (Basel). 2021-10-19

[4]
Functionality of apigenin as a potent antioxidant with emphasis on bioavailability, metabolism, action mechanism and in vitro and in vivo studies: A review.

J Food Biochem. 2022-4

[5]
Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities.

Mar Drugs. 2021-8-20

[6]
Does Oral Apigenin Have Real Potential for a Therapeutic Effect in the Context of Human Gastrointestinal and Other Cancers?

Front Pharmacol. 2021-5-18

[7]
Enhancing Oral Bioavailability of Apigenin Using a Bioactive Self-Nanoemulsifying Drug Delivery System (Bio-SNEDDS): In Vitro, In Vivo and Stability Evaluations.

Pharmaceutics. 2020-8-10

[8]
An Overview of Micro- and Nanoemulsions as Vehicles for Essential Oils: Formulation, Preparation and Stability.

Nanomaterials (Basel). 2020-1-12

[9]
Enhancement of zaleplon oral bioavailability using optimized self-nano emulsifying drug delivery systems and its effect on sleep quality among a sample of psychiatric patients.

Drug Deliv. 2019-12

[10]
Antioxidant and Photoprotective Activity of Apigenin and its Potassium Salt Derivative in Human Keratinocytes and Absorption in Caco-2 Cell Monolayers.

Int J Mol Sci. 2019-4-30

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