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解锁缓解之道:用于银屑病治疗的载水杨酸微乳凝胶的配方、表征及体内评估

Unlocking relief: formulation, characterization, and in vivo assessment of salicylic acid-loaded microemulgel for psoriasis management.

作者信息

Lotlikar Viswanath Baboy, Sharma Sanjay, Londhe Vaishali Y

机构信息

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, 400056, Maharashtra, India.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2025 Mar;398(3):3037-3047. doi: 10.1007/s00210-024-03447-3. Epub 2024 Sep 26.

DOI:10.1007/s00210-024-03447-3
PMID:39325151
Abstract

Psoriasis, a chronic skin condition, affects around 2-5% of the population. Topical corticosteroids treat the vast majority of cases (> 80%). Because of the physicochemical characteristics of the damaged stratum corneum, all treatments are ineffective. Nevertheless, systemic immunosuppression, the oral strategy, has substantial adverse effects that may be avoided using the topical procedure. The research sought to determine if a salicylic acid-loaded microemulsion-based gel (emulgel) could successfully infiltrate and maintain salicylic acid in skin tissue for psoriasis treatment. The pseudo-ternary phase was generated in different Smix ratios (1:1, 2:1, and 3:1; Labrasol:Transcutol® P). At a 3:1 ratio, the Smix had a substantial microemulsion area. Microemulsion was characterized for particle size, pH, etc. For topical application, the selected microemulsion was combined with Carbopol 940 gel, and ex vivo permeation and drug retention study were conducted. The effectiveness of the developed gel was checked using the IMQ-induced psoriatic plaque model. Salicylic acid microemulsion has an average globule size of 79.72 nm, pH 5.93, and 100% transmittance. In an ex vivo diffusion study, emulgel revealed greater penetration and more drug retention than ordinary salicylic acid gel. The emulgel was non-irritating on the skin of rats. In vivo studies revealed significant antipsoriatic activity of microemulsion-loaded gel compared to the marketed product. Developed emulgel was considered a potential product for an effective and safe way to administer salicylic acid for the treatment of skin diseases such as psoriasis.

摘要

银屑病是一种慢性皮肤疾病,影响着约2%-5%的人口。外用皮质类固醇可治疗绝大多数病例(>80%)。由于受损角质层的物理化学特性,所有治疗方法均无效。然而,全身免疫抑制这种口服策略具有大量不良反应,而采用局部用药程序则可避免这些不良反应。该研究旨在确定一种载有水杨酸的微乳凝胶(乳胶凝胶)能否成功渗透并在皮肤组织中维持水杨酸以用于银屑病治疗。在不同的表面活性剂混合物比例(1:1、2:1和3:1;Labrasol:Transcutol® P)下生成了伪三元相图。在3:1的比例下,表面活性剂混合物具有相当大的微乳区域。对微乳进行了粒径、pH值等方面的表征。对于局部应用,将选定的微乳与卡波姆940凝胶混合,并进行了离体渗透和药物滞留研究。使用咪喹莫特诱导的银屑病斑块模型检查了所开发凝胶的有效性。水杨酸微乳的平均球粒尺寸为79.72纳米,pH值为5.93,透光率为100%。在离体扩散研究中,乳胶凝胶显示出比普通水杨酸凝胶更大的渗透性和更多的药物滞留。该乳胶凝胶对大鼠皮肤无刺激性。体内研究表明,与市售产品相比,载有微乳的凝胶具有显著的抗银屑病活性。所开发的乳胶凝胶被认为是一种潜在的产品,可通过有效且安全的方式给药水杨酸来治疗银屑病等皮肤疾病。

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