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马霍塔德瓦(大果法勒利亚)种子提取物纳米乳剂剂型药理活性的改善:体外和体内研究

Improvement in Pharmacological Activity of Mahkota Dewa (Phaleria macrocarpa (Schef. Boerl)) Seed Extracts in Nanoemulsion Dosage Form: In Vitro and In Vivo Studies.

作者信息

Agustin Eriska, Insanu Muhammad, Mauludin Rachmat

机构信息

School of Pharmacy, Bandung Institute of Technology, Bandung 40132, Indonesia.

出版信息

Pharm Nanotechnol. 2023 Jun 2;12(1):90-7. doi: 10.2174/2211738511666230602100045.

Abstract

BACKGROUND

Mahkota Dewa (Phaleria macrocarpa) seed has various phytochemical compounds and low pharmacological activities, including antioxidant and anti-inflammatory activities.

OBJECTIVE

This research aimed to study nanoemulsion preparations of Mahkota Dewa seed (NE-BMD) for their anti-oxidant and anti-inflammatory properties.

METHOD

The nanoemulsion was prepared using an ultrasonication probe and followed by selecting two formulations, F7 and F8. The anti-oxidant activity test was carried out using the DPPH method, meanwhile, the anti-inflammatory activity test was conducted using the protein denaturation method with Bovine Serum Albumin (BSA) for in vitro studies. In addition, for in vivo studies, the plethysmometer method was used with 1% carrageenan as an inducer.

RESULTS

The characterization of NE-BMD preparations showed that the particle size and polydispersity index were 26,83 ± 1,27 nm (PI: 0.36 ± 0.03) and 30.73 ± 1.50 nm (PI: 0.32 ± 0.06) for NE-BMD F7 and F8 formulation, respectively. In addition, the anti-oxidant activity test revealed that the IC50 values of NE_BMD F7 and F8 were 15.62 ± 1.40 µg/ml and 28.39 ± 4.69 µg/ml, respectively. The protein denaturation test showed that the IC50 values for NE-BMD F7 and F8 were 94.39 ± 1.24 µg/ml and 196.63 ± 1.61 µg/ml, respectively. Meanwhile, the study of anti-inflammatory in vivo for NE-BMD F7 with a 1 g/kg BW dose showed a significant improvement in anti-inflammatory activity compared to BMD extract.

CONCLUSION

This research suggests that due to the smaller drug particle size, the nanoemulsion dosage form of Mahkota Dewa seed extract has anti-oxidant and anti-inflammatory activities, thus emerging as an adjunct alternative treatment for inflammation.

摘要

背景

美可多塔·德瓦(大果木竹子)种子含有多种植物化学成分,且具有较低的药理活性,包括抗氧化和抗炎活性。

目的

本研究旨在探讨美可多塔·德瓦种子纳米乳剂制剂(NE-BMD)的抗氧化和抗炎特性。

方法

使用超声探头制备纳米乳剂,然后选择两种制剂F7和F8。采用DPPH法进行抗氧化活性测试,同时采用蛋白质变性法,以牛血清白蛋白(BSA)进行体外抗炎活性测试。此外,在体内研究中,采用体积描记法,以1%角叉菜胶作为诱导剂。

结果

NE-BMD制剂的表征显示,NE-BMD F7和F8制剂的粒径和多分散指数分别为26.83±1.27nm(PI:0.36±0.03)和30.73±1.50nm(PI:0.32±0.06)。此外,抗氧化活性测试表明,NE_BMD F7和F8的IC50值分别为15.62±1.40μg/ml和28.39±4.69μg/ml。蛋白质变性测试表明,NE-BMD F7和F8的IC50值分别为94.39±1.24μg/ml和196.63±1.61μg/ml。同时,对剂量为1g/kg体重的NE-BMD F7进行的体内抗炎研究表明,与BMD提取物相比,其抗炎活性有显著改善。

结论

本研究表明,由于药物粒径较小,美可多塔·德瓦种子提取物的纳米乳剂剂型具有抗氧化和抗炎活性,因此有望成为炎症辅助替代治疗药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b70/10661950/d2545a60a201/PNT-12-90_F1.jpg

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