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制备并评估姜黄素脂质体的物理化学性质,以及评估它们在3T3和MCF-7细胞系中的细胞毒性。

Preparing and assessing the physiochemical properties of curcumin niosomes and evaluating their cytotoxicity in 3T3 and MCF-7 cell lines.

作者信息

Ashraf Ganjooei Narges, Ohadi Mandana, Mostafavi Seyyed Mohammad Amin, Behnam Behzad, Pardakhty Abbas

机构信息

Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran.

Herbal and Traditional Medicines Research Center, Kerman University of Medical Sciences, Kerman, Iran.

出版信息

Avicenna J Phytomed. 2021 Jul-Aug;11(4):417-427. doi: 10.22038/AJP.2021.18163.

Abstract

OBJECTIVE

Application of vesicular drug delivery systems has made major progress in pharmaceutical science and technology. Niosomal drug delivery is potentially efficient to improve the pharmacokinetic and pharmacological properties of many compounds. Curcumin (CUR) has several documented anticancer activities; however, it has a low bioavailability that necessitates the development of efficient delivery systems. Accordingly, different niosomal preparations were prepared and evaluated in the present study to find a suitable delivery system.

MATERIALS AND METHODS

Span and Tween 20, 40, 60, and 80 were employed with various concentrations of cholesterol for studying the ability to form curcumin-loaded niosomes. Multiple characterization techniques including visual evaluation, particle size analysis, stability, encapsulation efficiency (EE), and release profile were studied. Cytotoxicity of curcumin niosomes on MCF-7 and 3T3 cell lines was determined using MTT assay.

RESULTS

Visual and particle size analysis indicated the formation of seven niosomal formulations in the micron size range, while the formulation consisted of Tween 40/cholesterol (50/50 M%) with 0.05% w/v CUR had an average diameter of 475 nm. The latter formulation was selected and it had EE of 78.5%. The CUR release profile showed 18.7% release over a period of 300 min. The MTT results showed that CUR incorporation significantly increased the cytotoxicity of niosomes and the extent of toxicity was higher in MCF-7 cells.

CONCLUSION

In this study, a simple niosomal formulation was developed for CUR loading with favorable physicochemical properties. The presented niosomal curcumin had also considerable effects in cell toxicity studies, which can be suggested for future anticancer studies.

摘要

目的

囊泡药物递送系统在制药科学与技术领域已取得重大进展。非离子表面活性剂囊泡药物递送在改善许多化合物的药代动力学和药理学性质方面具有潜在的高效性。姜黄素(CUR)具有多项已被记录的抗癌活性;然而,其生物利用度较低,因此需要开发高效的递送系统。据此,本研究制备并评估了不同的非离子表面活性剂囊泡制剂,以找到合适的递送系统。

材料与方法

使用司盘以及吐温20、40、60和80与不同浓度的胆固醇来研究形成载姜黄素非离子表面活性剂囊泡的能力。研究了多种表征技术,包括外观评估、粒径分析、稳定性、包封率(EE)和释放曲线。使用MTT法测定姜黄素非离子表面活性剂囊泡对MCF - 7和3T3细胞系的细胞毒性。

结果

外观和粒径分析表明形成了七种微米尺寸范围的非离子表面活性剂囊泡制剂,而由吐温40/胆固醇(50/50摩尔%)与0.05% w/v CUR组成的制剂平均直径为475 nm。选择了后一种制剂,其包封率为78.5%。姜黄素释放曲线显示在300分钟内释放了18.7%。MTT结果表明,姜黄素的掺入显著增加了非离子表面活性剂囊泡的细胞毒性,且在MCF - 7细胞中的毒性程度更高。

结论

在本研究中,开发了一种用于负载姜黄素的简单非离子表面活性剂囊泡制剂,其具有良好的物理化学性质。所呈现的载姜黄素非离子表面活性剂囊泡在细胞毒性研究中也有显著效果,可用于未来的抗癌研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cd3/8264222/4ad5aa4a3ae6/AJP-11-417-g001.jpg

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