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基于维生素E的叶酸纳米乳剂:口服制剂配方及物理性质评估

Vitamin E-based Folic Acid Nanoemulsion: Formulation and Physical Evaluation for Oral Administration.

作者信息

Adi Annis Catur, Christanto Christanto, Rachmawati Heni, Adlia Amirah

机构信息

Faculty of Public Health, University of Airlangga, Kampus C Mulyorejo, Surabaya 60115, Indonesia.

School of Pharmacy, Bandung Institute of Technology, Ganesha 10, Bandung 40132, Indonesia.

出版信息

Pharm Nanotechnol. 2019;7(4):304-313. doi: 10.2174/2211738507666190717154040.

Abstract

BACKGROUND

Folic acid is essential in many metabolic processes and DNA synthesis. Nevertheless, folic acid is not stable, pH-sensitive, and deteriorated upon light exposure.

OBJECTIVE

This work was aimed to improve folic acid stability within vitamin E-based nanoemulsion.

METHODS

The nanoemulsion was prepared with self-nanoemulsification method by mixing vitamin E oil, Tween 20, and PEG 400. A pseudoternary phase diagram was constructed with aqueous titration to determine the optimum ratio for the mixture. The globule size, pH and entrapment efficiency were included in the nanoemulsion characterizations. In addition, the influence of centrifugation, storage, and pH on physical and chemical stabilities of folic acid nanoemulsion was evaluated.

RESULTS

Optimum formula was obtained from vitamin E, Tween 20, and PEG 400 with the ratio of 1:11:1, and the folic acid amount was 8 mg. The size of folic acidloaded oil globule was 15.10 ± 1.51 nm, and the nanoemulsion pH was 6.24 ± 0.01. The nanoemulsion system was able to load the folic acid completely. Folic acid in nanoemulsion was stable after 14 days at room temperature, and it was more stable compared to folic acid in solution. In addition, the physical and chemical characteristics of folic acid in nanoemulsion was not affected by the simulated gastric condition.

CONCLUSION

Hence, nanoemulsion is a promising strategy to enhance folic acid stability.

摘要

背景

叶酸在许多代谢过程和DNA合成中至关重要。然而,叶酸不稳定,对pH敏感,且光照后会变质。

目的

本研究旨在提高基于维生素E的纳米乳剂中叶酸的稳定性。

方法

采用自乳化法,将维生素E油、吐温20和聚乙二醇400混合制备纳米乳剂。通过水相滴定构建伪三元相图,以确定混合物的最佳比例。纳米乳剂的表征包括液滴大小、pH值和包封率。此外,还评估了离心、储存和pH值对叶酸纳米乳剂物理和化学稳定性的影响。

结果

维生素E、吐温20和聚乙二醇400的最佳配方比例为1:11:1,叶酸用量为8mg。载叶酸油滴大小为15.10±1.51nm,纳米乳剂pH值为6.24±0.01。纳米乳剂体系能够完全负载叶酸。纳米乳剂中的叶酸在室温下放置14天后稳定,与溶液中的叶酸相比更稳定。此外,纳米乳剂中叶酸的物理和化学特性不受模拟胃条件的影响。

结论

因此,纳米乳剂是提高叶酸稳定性的一种有前景的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b55/6967134/7aaa781c247f/PNT-7-304_F1.jpg

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