{"title":"胶囊包裹阿奇霉素和布洛芬，可在不同 pH 值下协同抗菌","authors":"Runliang Feng, Shiyu Chen, Yingshun Zhao, Mingzhu Wang, Yuli Li, Yunjing Jia, Zhimei Song","doi":"10.1007/s12247-024-09853-7","DOIUrl":null,"url":null,"abstract":"<div><h3>Purpose</h3><p>To improve azithromycin’s antibacterial activity at different pH through combination therapy.</p><h3>Method</h3><p>Azithromycin- and ibuprofen-loaded micelles were fabricated by the self-assembly of MPEG-PVL copolymer, respectively.</p><h3>Results</h3><p>The drug-loaded micelles had controlled drug release property with water-solubility improvement. Notably, at pH 7.4 or 6.0, the in vitro antibacterial experiments demonstrated that there was no synergistic effect for the two native drugs against <i>S. aureus</i>, but a significant synergy was observed when the two preparations were used in combination. In vitro PI fluorescence staining experiment demonstrated that the introduction of ibuprofen-loaded micelles obviously increased cellular uptake under low concentration of azithromycin-loaded micelles. Through SEM and spectral evaluation experiments, it was found that ibuprofen-loaded micelles could increase the cell permeability by interacting with proteins and phospholipids in the cell membrane, which was conducive to promoting azithromycin-loaded micelles to enter the cells and play a drug effect.</p><h3>Conclusion</h3><p>The azithromycin- and ibuprofen-loaded micelles with synergistically enhanced antibacterial activity are potential candidates for effective bacterial combination therapy.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 4","pages":""},"PeriodicalIF":2.7000,"publicationDate":"2024-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Micelles-Encapsulated with Azithromycin and Ibuprofen for Synergistic Antibacterial at Different pH\",\"authors\":\"Runliang Feng, Shiyu Chen, Yingshun Zhao, Mingzhu Wang, Yuli Li, Yunjing Jia, Zhimei Song\",\"doi\":\"10.1007/s12247-024-09853-7\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Purpose</h3><p>To improve azithromycin’s antibacterial activity at different pH through combination therapy.</p><h3>Method</h3><p>Azithromycin- and ibuprofen-loaded micelles were fabricated by the self-assembly of MPEG-PVL copolymer, respectively.</p><h3>Results</h3><p>The drug-loaded micelles had controlled drug release property with water-solubility improvement. Notably, at pH 7.4 or 6.0, the in vitro antibacterial experiments demonstrated that there was no synergistic effect for the two native drugs against <i>S. aureus</i>, but a significant synergy was observed when the two preparations were used in combination. In vitro PI fluorescence staining experiment demonstrated that the introduction of ibuprofen-loaded micelles obviously increased cellular uptake under low concentration of azithromycin-loaded micelles. Through SEM and spectral evaluation experiments, it was found that ibuprofen-loaded micelles could increase the cell permeability by interacting with proteins and phospholipids in the cell membrane, which was conducive to promoting azithromycin-loaded micelles to enter the cells and play a drug effect.</p><h3>Conclusion</h3><p>The azithromycin- and ibuprofen-loaded micelles with synergistically enhanced antibacterial activity are potential candidates for effective bacterial combination therapy.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>\",\"PeriodicalId\":656,\"journal\":{\"name\":\"Journal of Pharmaceutical Innovation\",\"volume\":\"19 4\",\"pages\":\"\"},\"PeriodicalIF\":2.7000,\"publicationDate\":\"2024-07-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Pharmaceutical Innovation\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s12247-024-09853-7\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Pharmaceutical Innovation","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s12247-024-09853-7","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
摘要
目的通过联合疗法提高阿奇霉素在不同pH值下的抗菌活性。方法利用MPEG-PVL共聚物的自组装技术分别制备了阿奇霉素和布洛芬载药胶束。值得注意的是，在 pH 值为 7.4 或 6.0 的条件下，体外抗菌实验表明两种原生药物对金黄色葡萄球菌没有协同作用，但当两种制剂联合使用时，则观察到了明显的协同作用。体外 PI 荧光染色实验表明，在低浓度阿奇霉素胶束的作用下，布洛芬胶束的引入明显增加了细胞的吸收。通过扫描电镜和光谱评价实验发现，布洛芬载药胶束能通过与细胞膜上的蛋白质和磷脂相互作用增加细胞的通透性，有利于促进阿奇霉素载药胶束进入细胞发挥药效。
Micelles-Encapsulated with Azithromycin and Ibuprofen for Synergistic Antibacterial at Different pH
Purpose
To improve azithromycin’s antibacterial activity at different pH through combination therapy.
Method
Azithromycin- and ibuprofen-loaded micelles were fabricated by the self-assembly of MPEG-PVL copolymer, respectively.
Results
The drug-loaded micelles had controlled drug release property with water-solubility improvement. Notably, at pH 7.4 or 6.0, the in vitro antibacterial experiments demonstrated that there was no synergistic effect for the two native drugs against S. aureus, but a significant synergy was observed when the two preparations were used in combination. In vitro PI fluorescence staining experiment demonstrated that the introduction of ibuprofen-loaded micelles obviously increased cellular uptake under low concentration of azithromycin-loaded micelles. Through SEM and spectral evaluation experiments, it was found that ibuprofen-loaded micelles could increase the cell permeability by interacting with proteins and phospholipids in the cell membrane, which was conducive to promoting azithromycin-loaded micelles to enter the cells and play a drug effect.
Conclusion
The azithromycin- and ibuprofen-loaded micelles with synergistically enhanced antibacterial activity are potential candidates for effective bacterial combination therapy.
期刊介绍：
The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories:
Materials science,
Product design,
Process design, optimization, automation and control,
Facilities; Information management,
Regulatory policy and strategy,
Supply chain developments ,
Education and professional development,
Journal of Pharmaceutical Innovation publishes four issues a year.
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