Intradermal delivery of teriflunomide loaded emulsomes using hollow microneedles for effective minimally invasive psoriasis management

IF 4.4 2区医学 Q1 PHARMACOLOGY & PHARMACY

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-03-11 DOI:10.1016/j.ejpb.2025.114692

Mariam Zewail , Haidy Abbas , Nesrine El Sayed , Heba Abd-El-Azim

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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.

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使用空心微针皮内递送特立氟米特负载乳剂用于有效的微创牛皮癣治疗

传统的局部银屑病治疗由于局部药物浓度高，对患处的递送有限以及皮肤刺激。本研究旨在改善来氟米特活性代谢物特氟米特（teriflunomide， TER）的递送，除了使用空心微针确保有效的皮内递送外，还可以通过纳米胶囊在乳剂（EMLs）中提高其溶解度。考察了EMLs的胶体特性、包封效率和释药效果。此外，通过测量炎症介质水平和解剖皮肤的组织病理学评估，评估吡喹莫德诱导银屑病小鼠模型的抗银屑病活性。所选EMLs配方的粒径为147.9 nm， zeta电位值为- 21.7。包封效率为97.23%，EMLs可持续释放48 h。经TER-EMLs处理的动物体内NF-KB、IL - 8、MMP1、GSH、SOD和过氧化氢酶水平与阴性对照组比较，差异均无统计学意义。此外，解剖皮肤样本的组织病理学检查也反映了TER- emls优于TER悬液。总的来说，纳米胶囊化和空心微针的应用改善了TER的性能，并确保了TER有效地输送到银屑病区。

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来源期刊

European Journal of Pharmaceutics and Biopharmaceutics 医学-药学

CiteScore

8.80

自引率

4.10%

发文量

211

审稿时长

36 days

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.