水飞蓟素表面修饰囊泡的制备:细胞活力评估的体外表征

IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Saudi Pharmaceutical Journal Pub Date : 2024-04-19 DOI:10.1016/j.jsps.2024.102072
Syed Sarim Imam, Sultan Owaid Alshammari, Sultan Alshehri, Wael A. Mahdi, Mohamed H. Al-Agamy
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引用次数: 0

摘要

水飞蓟素(SLR)是一种水溶性较差的生物活性化合物,具有广泛的治疗活性。本研究采用溶剂蒸发再水化法制备了纳米级水飞蓟素囊(F1-F6)。对水飞蓟素囊泡的大小、表面电荷、包埋效率和药物释放研究进行了评估。通过添加阳离子聚合物壳聚糖,对优化的 SLR 脂质囊(F3)进行了进一步修饰。随后,对改性后的囊泡(F3C1)进行了渗透通量、抗菌活性、细胞活力和分子对接研究评估。水飞蓟素囊泡的尺寸为纳米级(250 nm),多分散指数低(0.05),表面电荷为负,SLR截留率高(85-95%)。药物释放研究结果表明,最大药物释放率为 91.2 ± 2.8%。在表面添加壳聚糖后,其尺寸、多分散指数、表面电荷(正)和包封效率都发生了显著变化。与游离 SLR 相比,药物释放时间延长,渗透通量增加。与游离 SLR 和标准药物相比,抗菌效果更好。细胞活力测定也表明,F3C1 对细胞株的 IC50 值较低。
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Formulation of silymarin surface modified vesicles: In vitro characterization to cell viability assessment

Silymarin (SLR) is a poorly water-soluble bioactive compound with a wide range of therapeutic activities. Nanosized silymarin vesicles (F1–F6) were prepared by the solvent evaporation rehydration method. The silymarin vesicles were evaluated for vesicle size, surface charge, entrapment efficiency, and drug release studies. The optimized SLR lipid vesicle (F3) was further modified with the addition of the cationic polymer chitosan. After that, the modified vesicle (F3C1) was assessed for permeation flux, antimicrobial activity, cell viability, and molecular docking studies. The silymarin vesicles showed nanometric size (<250 nm), low polydispersibility index (<0.05), negative surface charge, and high SLR entrapment (85–95 %). The drug release study result demonstrated a maximum drug release of 91.2 ± 2.8 %. After adding chitosan to the surface, there was a significant change in the size, polydispersibility index, surface charge (positive), and encapsulation efficiency. The drug release was found to be prolonged, and the permeation flux was also increased in comparison to free SLR. A comparative antimicrobial result was observed in comparison to the free SLR and standard drug. The cell viability assay also demonstrated a low IC50 value for F3C1 against the cell line.

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来源期刊
Saudi Pharmaceutical Journal
Saudi Pharmaceutical Journal PHARMACOLOGY & PHARMACY-
CiteScore
6.10
自引率
2.40%
发文量
194
审稿时长
67 days
期刊介绍: The Saudi Pharmaceutical Journal (SPJ) is the official journal of the Saudi Pharmaceutical Society (SPS) publishing high quality clinically oriented submissions which encompass the various disciplines of pharmaceutical sciences and related subjects. SPJ publishes 8 issues per year by the Saudi Pharmaceutical Society, with the cooperation of the College of Pharmacy, King Saud University.
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