Microemulsion-Based Gel for Skin Delivery of Tacrolimus and Pramoxine Hydrochloride

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY

Journal of Pharmaceutical Innovation Pub Date : 2025-08-19 DOI:10.1007/s12247-025-10066-9

Janani Saravanan, K. V. Navyasree, Raiha Hareed, S. Swathi Krishna, Soumya Jagadeesan, Vidya Viswanad

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Abstract

AbstractSection Purpose

Atopic dermatitis (AD) is a chronic, pruritic skin disorder usually treated with topical tacrolimus and corticosteroids, which are limited by adverse effects such as burning sensations and allergic reactions. We developed a new microemulgel formulation combining tacrolimus with pramoxine hydrochloride, an anesthetic that reduces pruritus by inhibiting voltage-gated sodium channels. This study aimed to optimize the formulation to augment skin retention and permeation of tacrolimus, potentially enhancing therapeutic efficacy and addressing current treatment limitations for AD.

AbstractSection Methods

The microemulgel formulation was optimized using a mixture design. The formulation was evaluated for physicochemical properties, in vitro drug release, ex vivo skin permeation and retention, cell viability (MTT assay), and efficacy in reducing inflammatory mediators (RT-PCR).

AbstractSection Results

The optimized formulation exhibited a favorable release profile, with a rapid initial release of pramoxine hydrochloride for immediate local anesthetic effects, followed by sustained release of tacrolimus for prolonged therapeutic action. Ex vivo permeation studies using porcine skin indicated enhanced permeation and increased drug retention compared to a marketed ointment. Cytotoxicity assays confirmed formulation safety, with cell viability above 90% at therapeutic concentrations. RT-PCR analysis showed a significant reduction in IL-1α expression. Stability studies at various temperatures demonstrated long-term stability and integrity, making the formulation suitable for practical use.

AbstractSection Conclusions

The successfully prepared microemulsion-based gel of tacrolimus and pramoxine hydrochloride demonstrated improved skin permeation and skin retention. This dual drug-loaded microemulgel offers a promising approach for AD treatment, providing immediate relief and sustained therapeutic effect, potentially improving patient complaints and treatment outcomes.

AbstractSection Graphical Abstract

Abstract Image

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他克莫司和盐酸普拉莫辛皮肤递送微乳化凝胶

【摘要】特应性皮炎（AD）是一种慢性瘙痒性皮肤疾病，通常使用局部他克莫司和皮质类固醇治疗，但其不良反应如灼烧感和过敏反应有限。我们开发了一种新的微凝胶配方，结合了他克莫司和盐酸普拉莫辛，一种通过抑制电压门控钠通道来减少瘙痒的麻醉剂。本研究旨在优化配方，以增加他克莫司的皮肤保留和渗透，潜在地提高治疗效果，并解决目前治疗AD的局限性。【摘要】【章节】方法采用混合设计法对微乳的配方进行优化。评估了该制剂的理化性质、体外药物释放、体外皮肤渗透和保留、细胞活力（MTT法）和减少炎症介质的功效（RT-PCR）。【摘要】【部分】结果优化后的处方具有良好的释放特性，盐酸普拉莫辛初释放快速，可获得即时局部麻醉效果；他克莫司缓释，可延长治疗作用。体外渗透研究表明，与市场上销售的软膏相比，猪皮肤的渗透能力增强，药物潴留增加。细胞毒性试验证实了配方的安全性，在治疗浓度下细胞存活率超过90%。RT-PCR分析显示IL-1α表达明显降低。在不同温度下的稳定性研究证明了该配方的长期稳定性和完整性，使其适合实际使用。【摘要】结论制备的他克莫司-盐酸普拉莫辛微乳化凝胶具有良好的皮肤渗透性和皮肤潴留性。这种双重药物负载微凝胶为阿尔茨海默病的治疗提供了一种很有前途的方法，提供即时缓解和持续的治疗效果，有可能改善患者的抱怨和治疗结果。摘要节图形摘要

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

审稿时长

>12 weeks

期刊介绍： The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.