Antonela Bartolilla , Ariana Zoppi , Marcela R. Longhi , Virginia Aiassa
{"title":"克拉霉素-抗坏血酸的无载体胆固醇液晶和干凝胶具有增强的抗菌和抗生物膜活性","authors":"Antonela Bartolilla , Ariana Zoppi , Marcela R. Longhi , Virginia Aiassa","doi":"10.1016/j.ijpharm.2025.126255","DOIUrl":null,"url":null,"abstract":"<div><div>Antimicrobial resistance represents a worldwide problem that necessitates the creation of innovative pharmaceutical strategies. In this study, two carrier-free supramolecular systems composed exclusively of clarithromycin (CTY) and ascorbic acid (AA) were developed and characterized: a semi-solid amphotropic cholesteric liquid crystal (CLC) and a xerogel. The CLC gel represents the first report of a spontaneous and stable formation of a cholesteric phase from an antibiotic without additional structuring agents. Rheological studies and polarized light microscopy (PLM) show that the mesophase displayed typical viscoelastic behavior with both lyotropic and thermotropic features and consisted of nanometric particles with moderate uniformity, as confirmed by dynamic light scattering (DLS). The system enhanced the antibacterial activity of CTY. This was reflected in a lower minimum inhibitory concentration (MIC) and in the inhibition of <em>Staphylococcus aureus</em> biofilms, including clinical isolates. These findings highlight its potential use in topical or oral antibiotic formulations. The xerogel showed a lamellar organization, as revealed by the calculation of interplanar distances from the X-ray diffraction pattern and further supported by scanning electron microscopy (SEM). This system offers a novel and simple platform for the formulation of antibiotics.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"685 ","pages":"Article 126255"},"PeriodicalIF":5.2000,"publicationDate":"2025-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Carrier-free cholesteric liquid crystal and xerogel of clarithromycin-ascorbic acid with enhanced antimicrobial and antibiofilm activity\",\"authors\":\"Antonela Bartolilla , Ariana Zoppi , Marcela R. Longhi , Virginia Aiassa\",\"doi\":\"10.1016/j.ijpharm.2025.126255\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Antimicrobial resistance represents a worldwide problem that necessitates the creation of innovative pharmaceutical strategies. In this study, two carrier-free supramolecular systems composed exclusively of clarithromycin (CTY) and ascorbic acid (AA) were developed and characterized: a semi-solid amphotropic cholesteric liquid crystal (CLC) and a xerogel. The CLC gel represents the first report of a spontaneous and stable formation of a cholesteric phase from an antibiotic without additional structuring agents. Rheological studies and polarized light microscopy (PLM) show that the mesophase displayed typical viscoelastic behavior with both lyotropic and thermotropic features and consisted of nanometric particles with moderate uniformity, as confirmed by dynamic light scattering (DLS). The system enhanced the antibacterial activity of CTY. This was reflected in a lower minimum inhibitory concentration (MIC) and in the inhibition of <em>Staphylococcus aureus</em> biofilms, including clinical isolates. These findings highlight its potential use in topical or oral antibiotic formulations. The xerogel showed a lamellar organization, as revealed by the calculation of interplanar distances from the X-ray diffraction pattern and further supported by scanning electron microscopy (SEM). This system offers a novel and simple platform for the formulation of antibiotics.</div></div>\",\"PeriodicalId\":14187,\"journal\":{\"name\":\"International Journal of Pharmaceutics\",\"volume\":\"685 \",\"pages\":\"Article 126255\"},\"PeriodicalIF\":5.2000,\"publicationDate\":\"2025-10-08\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International Journal of Pharmaceutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0378517325010920\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Pharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0378517325010920","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Carrier-free cholesteric liquid crystal and xerogel of clarithromycin-ascorbic acid with enhanced antimicrobial and antibiofilm activity
Antimicrobial resistance represents a worldwide problem that necessitates the creation of innovative pharmaceutical strategies. In this study, two carrier-free supramolecular systems composed exclusively of clarithromycin (CTY) and ascorbic acid (AA) were developed and characterized: a semi-solid amphotropic cholesteric liquid crystal (CLC) and a xerogel. The CLC gel represents the first report of a spontaneous and stable formation of a cholesteric phase from an antibiotic without additional structuring agents. Rheological studies and polarized light microscopy (PLM) show that the mesophase displayed typical viscoelastic behavior with both lyotropic and thermotropic features and consisted of nanometric particles with moderate uniformity, as confirmed by dynamic light scattering (DLS). The system enhanced the antibacterial activity of CTY. This was reflected in a lower minimum inhibitory concentration (MIC) and in the inhibition of Staphylococcus aureus biofilms, including clinical isolates. These findings highlight its potential use in topical or oral antibiotic formulations. The xerogel showed a lamellar organization, as revealed by the calculation of interplanar distances from the X-ray diffraction pattern and further supported by scanning electron microscopy (SEM). This system offers a novel and simple platform for the formulation of antibiotics.
期刊介绍:
The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.