Preparation of oral nanoemulsion drug delivery system loaded with punicalagin: in vitro antibacterial activity, drug release, and cell safety studies

IF 2.8 4区 工程技术 Q2 POLYMER SCIENCE Macromolecular Research Pub Date : 2023-12-13 DOI:10.1007/s13233-023-00224-8
Fei-Fei Shi, Yu-Juan Mao, Ying Wang, Hai-Feng Yang
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Abstract

The objective of the present study was to develop a W/O/W nanoemulsion (NE) drug delivery system loaded with punicalagin (PGN) for oral delivery and evaluate its potential in antibacterial therapy. The W/O/W PGN-NE was prepared using a two-step process by combining ultrasonic with high-energy emulsification and subsequently characterized by its droplet size, zeta potential, and morphology. The PGN-NE was further evaluated for its pH, in vitro antibacterial activity, drug release property, and cytotoxicity. The results indicated the formation of spherical, nano-sized globules of PGN-NE had a mean particle size of 45.53 ± 2.2 nm, with a PDI value of 0.22 ± 0.028, zeta potential was −4.67 ± 0.88 mV, and pH value was 5.8. In vitro antibacterial activity studies showed a significantly higher antibacterial activity of PGN-NE in comparison to free PGN, suggesting that NE can effectively improve the antibacterial effect of natural pharmaceuticals. The drug release assay demonstrated that PGN was slowly released from the NE preparation and absorbed, helping to prolong the potency and improve the bioavailability of PGN. Cytotoxicity testing showed that PGN had reduced toxicity when encapsulated in NE. Thus, the developed NE formulation of PNG exhibited a greater potential for the slow-release effect delivery and in the treatment of microbial infections with favorable safety profile.

Graphical abstract

Micromorphology of W/O/W PGN nanoemulsion

The W/O/W PGN-NE are uniform in size and non-adhesive, with a size distribution of 28.214 to 141.772 nm and a mean size of 45.53 ± 2.2 nm, respectively, with a PDI value of 0.22 ± 0.028.

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制备含有潘立卡金的口服纳米乳液给药系统:体外抗菌活性、药物释放和细胞安全性研究
本研究的目的是开发一种口服给药的 W/O/W 纳米乳液(NE)给药系统,其中装载有 punicalagin (PGN),并评估其在抗菌治疗中的潜力。研究采用超声波和高能乳化两步法制备了 W/O/W PGN-NE,随后对其液滴大小、ZETA电位和形态进行了表征。对 PGN-NE 的 pH 值、体外抗菌活性、药物释放特性和细胞毒性进行了进一步评估。结果表明,PGN-NE 形成了球形纳米大小的球体,平均粒径为 45.53 ± 2.2 nm,PDI 值为 0.22 ± 0.028,zeta 电位为 -4.67 ± 0.88 mV,pH 值为 5.8。体外抗菌活性研究表明,PGN-NE 的抗菌活性明显高于游离 PGN,这表明 NE 能有效提高天然药物的抗菌效果。药物释放试验表明,PGN 可从 NE 制剂中缓慢释放并被吸收,这有助于延长 PGN 的药效并提高其生物利用度。细胞毒性测试表明,将 PGN 封装在 NE 中可降低其毒性。图解摘要W/O/W PGN 纳米乳液的微形貌W/O/W PGN-NE 尺寸均匀且无粘性,尺寸分布为 28.214 至 141.772 nm,平均尺寸为 45.53 ± 2.2 nm,PDI 值为 0.22 ± 0.028。
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来源期刊
Macromolecular Research
Macromolecular Research 工程技术-高分子科学
CiteScore
4.70
自引率
8.30%
发文量
100
审稿时长
1.3 months
期刊介绍: Original research on all aspects of polymer science, engineering and technology, including nanotechnology Presents original research articles on all aspects of polymer science, engineering and technology Coverage extends to such topics as nanotechnology, biotechnology and information technology The English-language journal of the Polymer Society of Korea Macromolecular Research is a scientific journal published monthly by the Polymer Society of Korea. Macromolecular Research publishes original researches on all aspects of polymer science, engineering, and technology as well as new emerging technologies using polymeric materials including nanotechnology, biotechnology, and information technology in forms of Articles, Communications, Notes, Reviews, and Feature articles.
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