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纳米乳剂制剂的制备及根和地上部分提取物的表征:纳米乳剂与纯植物提取物的抗菌和抗癌活性评价。

Preparation and characterization of nano-emulsion formulations of root and aerial parts extracts: evaluation of antibacterial and anticancer activities of nano-emulsion versus pure plant extract.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Helwan University. Ain Helwan, Cairo, Egypt.

Microbiology Department, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt.

出版信息

Drug Dev Ind Pharm. 2024 Jul;50(7):658-670. doi: 10.1080/03639045.2024.2386001. Epub 2024 Aug 6.

DOI:10.1080/03639045.2024.2386001
PMID:39093556
Abstract

OBJECTIVE

Preparation and characterization of nano-emulsion formulations for aerial and root parts extracts.

SIGNIFICANCE

Genus Asparagus is known for its antimicrobial and anticancer activities, however, freeze dried powder of aqueous - alcoholic extract prepared in this study, exhibited a limited water solubility, limiting its therapeutic application. Thus, encapsulation of its phytochemicals into nano-emulsion is proposed as a solution to improve water solubility, and facilitate its clinical translation.

METHODS

the composition of extracts for both aerial and root parts of was identified by HPLC and LC-MS analysis. Nano-emulsion was prepared homogenization where a mixture of Castor oil: phosphate buffered saline (10 mM, pH 7.4): Tween 80: PEG 600 in a ratio of 10: 5: 2.5: 2.5, respectively. Nano-emulsion formulations were characterized for particle size, polydispersity index (PDI), zeta potential, TEM, viscosity and pH. Then, the antibacterial and anticancer activities of nano-emulsion formulations versus their pure plant counterparts was assessed.

RESULTS

The analysis of extracts identified several flavonoids, phenolics, and saponins which were reported to have antimicrobial and anticancer activities. Nano-emulsion formulations were monodispersed with droplet sizes ranging from 80.27 ± 2.05 to 111.16 ± 1.97 nm, and polydispersity index ≤0.3. Nano-emulsion formulations enhanced significantly the antibacterial (multidrug resistant bacteria causing skin and dental soft tissues infections) and anticancer (HuH7, HEPG2, H460 and HCT116) activities compared to their pure plant extract counterparts.

CONCLUSION

Employing a nano-delivery system as a carrier for phytochemicals might be an effective strategy to enhance their pharmacological activity, overcome their limitations, and ultimately increase their potential for clinical applications.

摘要

目的

制备和表征空气部分和根部提取物的纳米乳液制剂。

意义

天门冬属因其具有抗菌和抗癌活性而闻名,然而,本研究中制备的水-醇提物的冷冻干燥粉末表现出有限的水溶性,限制了其治疗应用。因此,将其植物化学物质包封到纳米乳液中被提议为一种提高水溶性并促进其临床转化的解决方案。

方法

通过 HPLC 和 LC-MS 分析鉴定了空气部分和根部提取物的成分。纳米乳液通过均质法制备,其中蓖麻油:磷酸盐缓冲盐水(10 mM,pH 7.4):吐温 80:聚乙二醇 600 的比例分别为 10:5:2.5:2.5。分别对纳米乳液制剂的粒径、多分散指数(PDI)、Zeta 电位、TEM、粘度和 pH 值进行了表征。然后,评估了纳米乳液制剂与纯植物制剂相比的抗菌和抗癌活性。

结果

提取物分析鉴定了几种被报道具有抗菌和抗癌活性的类黄酮、酚类和皂苷。纳米乳液制剂呈单分散状态,粒径范围为 80.27±2.05 至 111.16±1.97nm,多分散指数≤0.3。与纯植物提取物相比,纳米乳液制剂显著增强了抗菌(引起皮肤和牙齿软组织感染的多药耐药菌)和抗癌(HuH7、HEPG2、H460 和 HCT116)活性。

结论

将纳米递药系统作为植物化学物质的载体可能是一种有效的策略,可以增强其药理活性,克服其局限性,并最终增加其临床应用潜力。

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