{"title":"Everolimus-encapsulation in Pluronic P123 self-assembled micelles as drug delivery systems for drug-coated balloons","authors":"Mohammad Akrami-Hasan-Kohal , Adrien Chouchou , Sébastien Blanquer , Tahmer Sharkawi","doi":"10.1016/j.ijpx.2024.100230","DOIUrl":null,"url":null,"abstract":"<div><p>Drug-coated balloons (DCBs) are effective tools for cardiovascular interventions, ensuring uniform drug delivery to occluded arteries. This research investigates the potential of Pluronic P123 (P123), a micelle-forming polymer, to solubilize and release Everolimus (EVE) from DCBs. Furthermore, it seeks to understand how the ratio of P123 to EVE affects release rates and micelle formation under physiological conditions. We tested three P123 to EVE ratios: 90:10, 75:25, and 50:50. Microscopy revealed that increasing EVE proportions resulted in more uniform coatings. Fourier-transform infrared spectroscopy (FTIR) analysis confirmed the successful incorporation of EVE into the P123 matrix without altering its chemical properties. Differential scanning calorimetry (DSC) studies showed that EVE incorporation affected the crystalline structure of P123, leading to more uniform coatings. In vitro release studies showed that all formulations had <1% drug loss in the first minute (the tracking phase); furthermore, the 90:10 ratio exhibited optimal drug release in the following 3 min, corresponding to the deployment phase in DCB angioplasty. Analysis of micelle loading capacity (LC), encapsulation efficiency (EE), size, and structure indicated an increase in both LC and EE with higher EVE content and a corresponding enlargement in micelle size. Given these findings, the optimized formula provided a consistent coating on commercial balloons, highlighting the potential of using P123 for DCB drug coating and release.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100230"},"PeriodicalIF":5.2000,"publicationDate":"2024-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000021/pdfft?md5=c594d2ed3f793f14634838a04c5b3943&pid=1-s2.0-S2590156724000021-main.pdf","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Pharmaceutics: X","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2590156724000021","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
Abstract
Drug-coated balloons (DCBs) are effective tools for cardiovascular interventions, ensuring uniform drug delivery to occluded arteries. This research investigates the potential of Pluronic P123 (P123), a micelle-forming polymer, to solubilize and release Everolimus (EVE) from DCBs. Furthermore, it seeks to understand how the ratio of P123 to EVE affects release rates and micelle formation under physiological conditions. We tested three P123 to EVE ratios: 90:10, 75:25, and 50:50. Microscopy revealed that increasing EVE proportions resulted in more uniform coatings. Fourier-transform infrared spectroscopy (FTIR) analysis confirmed the successful incorporation of EVE into the P123 matrix without altering its chemical properties. Differential scanning calorimetry (DSC) studies showed that EVE incorporation affected the crystalline structure of P123, leading to more uniform coatings. In vitro release studies showed that all formulations had <1% drug loss in the first minute (the tracking phase); furthermore, the 90:10 ratio exhibited optimal drug release in the following 3 min, corresponding to the deployment phase in DCB angioplasty. Analysis of micelle loading capacity (LC), encapsulation efficiency (EE), size, and structure indicated an increase in both LC and EE with higher EVE content and a corresponding enlargement in micelle size. Given these findings, the optimized formula provided a consistent coating on commercial balloons, highlighting the potential of using P123 for DCB drug coating and release.
期刊介绍:
International Journal of Pharmaceutics: X offers authors with high-quality research who want to publish in a gold open access journal the opportunity to make their work immediately, permanently, and freely accessible.
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The International Journal of Pharmaceutics is the second most cited journal in the "Pharmacy & Pharmacology" category out of 358 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.