Preparation of 5-ASA-loaded Eudragit® S100 nanoparticles by emulsion-based methods: Comparison between solvent evaporation and supercritical fluid extraction

IF 4.4 3区工程技术 Q2 CHEMISTRY, PHYSICAL

Journal of Supercritical Fluids Pub Date : 2025-08-20 DOI:10.1016/j.supflu.2025.106753

David Vizcaya , Diego F. Tirado , Albertina Cabañas , Dolores R. Serrano , Lourdes Calvo

{"title":"Preparation of 5-ASA-loaded Eudragit® S100 nanoparticles by emulsion-based methods: Comparison between solvent evaporation and supercritical fluid extraction","authors":"David Vizcaya , Diego F. Tirado , Albertina Cabañas , Dolores R. Serrano , Lourdes Calvo","doi":"10.1016/j.supflu.2025.106753","DOIUrl":null,"url":null,"abstract":"<div><div>Breaking away from the limitations of conventional solvent evaporation (SE), supercritical fluid extraction of emulsions (SFEE) offers a transformative approach to the production of polymeric nanoparticles. In this study, both SFEE and SE were applied to formulate nanoparticles composed of Eudragit® S100 loaded with 5-aminosalicylic acid (5-ASA), a drug widely used in the treatment of inflammatory bowel disease (IBD). A comparison was made between the two methods in terms of particle size distribution, encapsulation efficiency, residual solvent content, and morphology. Formulation efforts focused on obtaining a stable emulsion. A mixed organic phase was required: acetone to dissolve the polymer and a second solvent to solubilise the drug, underscoring the formulation challenge. Among the solvents evaluated, dimethyl sulfoxide (DMSO) was selected due to its ability to maximise 5-ASA solubility, enhance emulsion stability, and its classification as a low-risk Class 3 solvent. SFEE resulted in larger particle sizes (D50 = 165 nm) and slightly lower encapsulation efficiency (<em>EE</em> = 84 %) compared to SE (D50 = 85 nm, <em>EE</em> = 99 %). Despite the high boiling point of DMSO, SFEE achieved a significant reduction in residual solvent content (< 4 %) versus 21 % in SE particles. Both particles showed similar release profiles, with a rapid release of 5-ASA under acidic conditions despite being formulated with a pH-sensitive polymer. This behaviour was likely attributed to the nanometric size and high surface area of the particles, which favoured rapid drug diffusion.</div></div>","PeriodicalId":17078,"journal":{"name":"Journal of Supercritical Fluids","volume":"227 ","pages":"Article 106753"},"PeriodicalIF":4.4000,"publicationDate":"2025-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Supercritical Fluids","FirstCategoryId":"5","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0896844625002402","RegionNum":3,"RegionCategory":"工程技术","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, PHYSICAL","Score":null,"Total":0}

引用次数: 0

Abstract

Breaking away from the limitations of conventional solvent evaporation (SE), supercritical fluid extraction of emulsions (SFEE) offers a transformative approach to the production of polymeric nanoparticles. In this study, both SFEE and SE were applied to formulate nanoparticles composed of Eudragit® S100 loaded with 5-aminosalicylic acid (5-ASA), a drug widely used in the treatment of inflammatory bowel disease (IBD). A comparison was made between the two methods in terms of particle size distribution, encapsulation efficiency, residual solvent content, and morphology. Formulation efforts focused on obtaining a stable emulsion. A mixed organic phase was required: acetone to dissolve the polymer and a second solvent to solubilise the drug, underscoring the formulation challenge. Among the solvents evaluated, dimethyl sulfoxide (DMSO) was selected due to its ability to maximise 5-ASA solubility, enhance emulsion stability, and its classification as a low-risk Class 3 solvent. SFEE resulted in larger particle sizes (D50 = 165 nm) and slightly lower encapsulation efficiency (EE = 84 %) compared to SE (D50 = 85 nm, EE = 99 %). Despite the high boiling point of DMSO, SFEE achieved a significant reduction in residual solvent content (< 4 %) versus 21 % in SE particles. Both particles showed similar release profiles, with a rapid release of 5-ASA under acidic conditions despite being formulated with a pH-sensitive polymer. This behaviour was likely attributed to the nanometric size and high surface area of the particles, which favoured rapid drug diffusion.

查看原文本刊更多论文

乳化法制备5- asa负载的Eudragit®S100纳米颗粒：溶剂蒸发与超临界流体萃取的比较

超临界流体萃取（SFEE）技术突破了传统溶剂蒸发（SE）技术的局限性，为聚合物纳米颗粒的生产提供了一种革命性的方法。在这项研究中，SFEE和SE被应用于制备由Eudragit®S100组成的纳米颗粒，该纳米颗粒负载5-氨基水杨酸（5-ASA），这是一种广泛用于治疗炎症性肠病（IBD）的药物。从粒径分布、包封效率、残留溶剂含量、形貌等方面对两种方法进行了比较。配方工作的重点是获得稳定的乳液。需要一种混合的有机相：丙酮溶解聚合物，第二种溶剂溶解药物，这强调了配方的挑战。在评估的溶剂中，之所以选择二甲基亚砜（DMSO），是因为它能够最大限度地提高5-ASA的溶解度，增强乳液的稳定性，并且被归类为低风险的3类溶剂。与SE （D50 = 85nm, EE = 99%）相比，SFEE的粒径更大（D50 = 165nm），封装效率（EE = 84%）略低。尽管DMSO的沸点很高，但SFEE显著降低了残余溶剂含量（4%），而SE颗粒则降低了21%。两种颗粒均表现出相似的释放特性，尽管采用ph敏感聚合物配制，但在酸性条件下仍能快速释放5-ASA。这种行为可能归因于颗粒的纳米尺寸和高表面积，这有利于药物的快速扩散。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Journal of Supercritical Fluids 工程技术-工程：化工

CiteScore

7.60

自引率

10.30%

发文量

236

审稿时长

56 days

期刊介绍： The Journal of Supercritical Fluids is an international journal devoted to the fundamental and applied aspects of supercritical fluids and processes. Its aim is to provide a focused platform for academic and industrial researchers to report their findings and to have ready access to the advances in this rapidly growing field. Its coverage is multidisciplinary and includes both basic and applied topics. Thermodynamics and phase equilibria, reaction kinetics and rate processes, thermal and transport properties, and all topics related to processing such as separations (extraction, fractionation, purification, chromatography) nucleation and impregnation are within the scope. Accounts of specific engineering applications such as those encountered in food, fuel, natural products, minerals, pharmaceuticals and polymer industries are included. Topics related to high pressure equipment design, analytical techniques, sensors, and process control methodologies are also within the scope of the journal.