Mariam Zewail , Haidy Abbas , Nesrine El Sayed , Heba Abd-El-Azim
{"title":"Intradermal delivery of teriflunomide loaded emulsomes using hollow microneedles for effective minimally invasive psoriasis management","authors":"Mariam Zewail , Haidy Abbas , Nesrine El Sayed , Heba Abd-El-Azim","doi":"10.1016/j.ejpb.2025.114692","DOIUrl":null,"url":null,"abstract":"<div><div>Conventional topical psoriasis treatments suffer from limited delivery to affected areas along with skin irritation due to high local drug concentration. Herein an attempt to improve the delivery of leflunomide’s active metabolite (teriflunomide (TER)) by improving its solubility through nanoencapsulation in emulsomes (EMLs) besides ensuring effective intradermal delivery using hollow microneedles. Evaluation of colloidal characteristics of EMLs, encapsulation efficiency and drug release were performed. Additionally, the antipsoriatic activity in an imiquimod-induced psoriatic mouse model was evaluated by the measurement of inflammatory mediators’ levels and histopathological assessment of anatomized skin. The particle size of the chosen EMLs formulation was 147.9 nm and the zeta potential value was −21.7. Entrapment efficiency was 97.23 % and EMLs provided sustained drug release for 48 h. No statistically significant differences in the <em>in vivo</em> levels of NF-KB, IL 8, MMP1, GSH, SOD and catalase between the animals treated by TER-EMLs and the negative control cohort were observed. Also, histopathological inspection of dissected skin samples reflected the superiority of TER-EMLs over TER suspension. Collectively, combining nanoencapsulation and hollow microneedles application improved TER properties and ensured effective TER delivery to the affected psoriatic areas.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"210 ","pages":"Article 114692"},"PeriodicalIF":4.4000,"publicationDate":"2025-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Pharmaceutics and Biopharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0939641125000682","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
Conventional topical psoriasis treatments suffer from limited delivery to affected areas along with skin irritation due to high local drug concentration. Herein an attempt to improve the delivery of leflunomide’s active metabolite (teriflunomide (TER)) by improving its solubility through nanoencapsulation in emulsomes (EMLs) besides ensuring effective intradermal delivery using hollow microneedles. Evaluation of colloidal characteristics of EMLs, encapsulation efficiency and drug release were performed. Additionally, the antipsoriatic activity in an imiquimod-induced psoriatic mouse model was evaluated by the measurement of inflammatory mediators’ levels and histopathological assessment of anatomized skin. The particle size of the chosen EMLs formulation was 147.9 nm and the zeta potential value was −21.7. Entrapment efficiency was 97.23 % and EMLs provided sustained drug release for 48 h. No statistically significant differences in the in vivo levels of NF-KB, IL 8, MMP1, GSH, SOD and catalase between the animals treated by TER-EMLs and the negative control cohort were observed. Also, histopathological inspection of dissected skin samples reflected the superiority of TER-EMLs over TER suspension. Collectively, combining nanoencapsulation and hollow microneedles application improved TER properties and ensured effective TER delivery to the affected psoriatic areas.
期刊介绍:
The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics.
Topics covered include for example:
Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids)
Aspects of manufacturing process design
Biomedical aspects of drug product design
Strategies and formulations for controlled drug transport across biological barriers
Physicochemical aspects of drug product development
Novel excipients for drug product design
Drug delivery and controlled release systems for systemic and local applications
Nanomaterials for therapeutic and diagnostic purposes
Advanced therapy medicinal products
Medical devices supporting a distinct pharmacological effect.