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采用 UPLC-MS/MS 方法对南洋杉提取物进行标准化和定量分析,并将其制成具有抗菌作用的植物纳米乳液凝胶。

Standardization and quantitative analysis of Araucaria Heterophylla extract via an UPLC-MS/MS method and its formulation as an antibacterial phytonanoemulsion gel.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Ahram Candian University, 6 October, Cairo, Egypt.

Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Ahram Canadian University, 6 October, Cairo, Egypt.

出版信息

Sci Rep. 2022 Jul 22;12(1):12557. doi: 10.1038/s41598-022-16188-1.

DOI:10.1038/s41598-022-16188-1
PMID:35869113
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9307656/
Abstract

Skin infections are among the bacterial infections that present significant therapeutic challenges due to antibiotic resistance. Recently, herbal products clutched a significant attention as safe replacements for other medications but their low aqueous solubility and poor bioavailability are considered major challenges which could be circumvented via formulation. As a species of genera Araucaria, Araucaria Heterophylla possesses pharmacological activities such as antioxidant and antibacterial actions, and this study aimed to standardize the extract of the plant against 4'''methoxyamentoflavone (as a main component of the extract) through a validated UPLC-MS/MS method and evaluate its antibacterial activity, which was followed by loading the standardized extract into a nanoemulsion to form a phytonanoemulsion (PNE), where the design analysis and optimization were performed through a simplex lattice design. The optimized PNE (PNE 3) was then loaded into HPMC/Pluronic F-127 gel (in ratio 1:4) to sustain the release of the active constituent. The heightened penetrability of PNE 3 gel was visualized via confocal laser scanning microscopy, and its prolonged effect was proved thru an in vivo study conducted on male Wistar rats. A histopathological study revealed the safety of the formulation when applied topically. Thus, PNE gel could be a potentially broad-spectrum antibacterial drug delivery system.

摘要

皮肤感染是由于抗生素耐药性而导致治疗极具挑战性的细菌性感染之一。最近,草药产品作为其他药物的安全替代品引起了广泛关注,但它们的低水溶解度和差的生物利用度被认为是主要挑战,可以通过制剂来规避。作为南洋杉属的一个物种,南洋杉 Heterophylla 具有药理学活性,如抗氧化和抗菌作用,本研究旨在通过经过验证的 UPLC-MS/MS 方法对该植物的提取物进行 4'''甲氧基安息香素(作为提取物的主要成分)的标准化,并评估其抗菌活性,随后将标准化提取物载入纳米乳剂中形成植物纳米乳剂(PNE),通过单形格子设计对其进行设计分析和优化。然后将优化后的 PNE(PNE3)载入 HPMC/Pluronic F-127 凝胶(比例为 1:4)中以维持活性成分的释放。通过共聚焦激光扫描显微镜观察到 PNE3 凝胶的渗透性增强,并通过对雄性 Wistar 大鼠进行的体内研究证明了其长效作用。组织病理学研究表明,该制剂局部应用时具有安全性。因此,PNE 凝胶可能是一种有潜力的广谱抗菌药物传递系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/654dcd8d3c03/41598_2022_16188_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/d2f411fb2143/41598_2022_16188_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/1735d1e4f977/41598_2022_16188_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/ff36e8ca79f0/41598_2022_16188_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/654dcd8d3c03/41598_2022_16188_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/d2f411fb2143/41598_2022_16188_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/1735d1e4f977/41598_2022_16188_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/ff36e8ca79f0/41598_2022_16188_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/822b/9307656/654dcd8d3c03/41598_2022_16188_Fig4_HTML.jpg

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