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褐藻糖胶基聚乙二醇化 PLGA 纳米粒包封甲基氨茴酸的研究进展：体外评价及体内抗炎研究。

Insight into Fucoidan-Based PEGylated PLGA Nanoparticles Encapsulating Methyl Anthranilic Acid: In Vitro Evaluation and In Vivo Anti-Inflammatory Study.

机构信息

Pharmaceutical Technology Department, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt.

Pharmaceutical Microbiology Department, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt.

出版信息

Mar Drugs. 2022 Nov 4;20(11):694. doi: 10.3390/md20110694.

DOI:10.3390/md20110694
PMID:36355017
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9693061/
Abstract

A potential fucoidan-based PEGylated PLGA nanoparticles (NPs) offering a proper delivery of -methyl anthranilic acid (MA, a model of hydrophobic anti-inflammatory drug) have been developed via the formation of fucoidan aqueous coating surrounding PEGylated PLGA NPs. The optimum formulation (FuP2) composed of fucoidan:m-PEG-PLGA (1:0.5 ) with particle size (365 ± 20.76 nm), zeta potential (-22.30 ± 2.56 mV), % entrapment efficiency (85.45 ± 7.41), drug loading (51.36 ± 4.75 µg/mg of NPs), % initial burst (47.91 ± 5.89), and % cumulative release (102.79 ± 6.89) has been further investigated for the anti-inflammatory in vivo study. This effect of FuP2 was assessed in rats' carrageenan-induced acute inflammation model. The average weight of the paw edema was significantly lowered ( ≤ 0.05) by treatment with FuP2. Moreover, cyclooxygenase-2 and tumor necrosis factor-alpha immunostaining were decreased in FuP2 treated group compared to the other groups. The levels of prostaglandin E2, nitric oxide, and malondialdehyde were significantly reduced ( ≤ 0.05) in the FuP2-treated group. A significant reduction ( ≤ 0.05) in the expression of interleukins (IL-1 and IL-6) with an improvement of the histological findings of the paw tissues was observed in the FuP2-treated group. Thus, fucoidan-based PEGylated PLGA-MA NPs are a promising anti-inflammatory delivery system that can be applied for other similar drugs potentiating their pharmacological and pharmacokinetic properties.

摘要

一种潜在的基于岩藻聚糖的聚乙二醇化 PLGA 纳米粒子（NPs），通过形成岩藻聚糖水涂层包围聚乙二醇化 PLGA NPs，提供了 -甲基氨茴酸（MA，一种疏水性抗炎药物的模型）的适当递送。最佳配方（FuP2）由岩藻聚糖：m-PEG-PLGA（1:0.5）组成，粒径（365 ± 20.76nm），Zeta 电位（-22.30 ± 2.56mV），%包封效率（85.45 ± 7.41），药物载量（51.36 ± 4.75µg/mg NPs），%初始突释（47.91 ± 5.89）和%累积释放（102.79 ± 6.89），进一步研究了其体内抗炎作用。在大鼠角叉菜胶诱导的急性炎症模型中评估了 FuP2 的这种作用。FuP2 治疗组的爪肿胀平均重量显著降低（≤0.05）。此外，与其他组相比，FuP2 处理组的环氧合酶-2 和肿瘤坏死因子-α免疫染色减少。FuP2 治疗组前列腺素 E2、一氧化氮和丙二醛水平显著降低（≤0.05）。FuP2 治疗组白细胞介素（IL-1 和 IL-6）的表达显著降低（≤0.05），爪组织的组织学发现得到改善。因此，基于岩藻聚糖的聚乙二醇化 PLGA-MA NPs 是一种有前途的抗炎药物递送系统，可应用于其他类似药物，增强其药理和药代动力学特性。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d896/9693061/f351ed72daef/marinedrugs-20-00694-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d896/9693061/28a9be390e1c/marinedrugs-20-00694-g009.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d896/9693061/10f90c7bffad/marinedrugs-20-00694-g012.jpg

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