Development and Characterization of Sulfasalazine Cubosomes for Potential Transdermal Drug Delivery.

Q2 Pharmacology, Toxicology and Pharmaceutics Pharmaceutical nanotechnology Pub Date : 2025-01-01 DOI:10.2174/0122117385269522231113041029

Mekha Mathew, Anasuya Patil, Hemanth G

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Abstract

Background: Rheumatoid arthritis is indeed a constant, progressive autoimmune disease that acts on the synovial membrane, distinguished by joint pain, swelling, and tenderness. Sulfasalazine belongs to BCS Class IV having low solubility and low permeability. To overcome the issue and provide a localized effect Cubosomes were chosen for the transdermal drug delivery system.

Objectives: The primary objective of this investigation was to pass on sulfasalazine-loaded cubosomes over the skin to treat rheumatoid arthritis. On the way to overcome this issue of oral sulfasalazine and provide localized effect, Cubosomes were chosen for the transdermal drug delivery system.

Methods: Sulfasalazine-loaded cubosomes were prepared by the top-down method using GMO and Poloxamer 407. Different concentrations of lipid and surfactant were used in the formulation using 3² full factorial designs. The prepared formulations were assessed for p.s, z,p, %EE, FTIR, SEM, in-vitro release, ex-vivo permeation, and deposition studies with pH 7.4 phosphate buffer saline.

Results: The particle size varies between 65 nm to 129 nm, while the negative zeta potential ranged from - 18.8 mV to -24.8 mV. The entrapment efficiency was between 87% and 95%. The formulations' in-vitro drug release was carried out for 12 hours. The optimized formulation showed a controlled release of sulfasalazine and better ex-vivo permeation and deposition properties than sulfasalazine suspension.

Conclusion: Overall study findings support the possibility of applying transdermal sulfasalazineloaded cubosomes to alleviate rheumatoid arthritis.

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用于潜在透皮给药的磺胺柳氮立方体的开发与表征

背景：类风湿性关节炎是一种作用于滑膜的持续性、进行性自身免疫性疾病，主要表现为关节疼痛、肿胀和压痛。磺胺属于 BCS IV 类，具有低溶解性和低渗透性。为了克服这一问题，并提供局部效果，我们选择了 Cubosomes 作为透皮给药系统：这项研究的主要目的是将含有磺胺的立方体通过皮肤来治疗类风湿性关节炎。为了克服口服磺胺的问题并提供局部疗效，我们选择了立方体作为透皮给药系统：方法：使用 GMO 和 Poloxamer 407 通过自上而下的方法制备了装载磺胺的立方体。采用 32 种全因子设计，在配方中使用了不同浓度的脂质和表面活性剂。对制备的制剂进行了 p.s、z,p、%EE、傅立叶变换红外光谱、扫描电子显微镜、体外释放、体外渗透和 pH 值为 7.4 的磷酸盐缓冲盐水沉积研究：粒径在 65 纳米到 129 纳米之间，负 zeta 电位在 -18.8 mV 到 -24.8 mV 之间。夹带效率在 87% 至 95% 之间。配方的体外药物释放时间为 12 小时。与磺胺沙拉嗪混悬液相比，优化后的配方显示出磺胺沙拉嗪的控释以及更好的体内外渗透和沉积特性：总体研究结果表明，透皮柳氮磺胺吡啶负载立方体可用于缓解类风湿性关节炎。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Pharmaceutical nanotechnology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

4.20

自引率

0.00%

发文量

期刊介绍： Pharmaceutical Nanotechnology publishes original manuscripts, full-length/mini reviews, thematic issues, rapid technical notes and commentaries that provide insights into the synthesis, characterisation and pharmaceutical (or diagnostic) application of materials at the nanoscale. The nanoscale is defined as a size range of below 1 µm. Scientific findings related to micro and macro systems with functionality residing within features defined at the nanoscale are also within the scope of the journal. Manuscripts detailing the synthesis, exhaustive characterisation, biological evaluation, clinical testing and/ or toxicological assessment of nanomaterials are of particular interest to the journal’s readership. Articles should be self contained, centred around a well founded hypothesis and should aim to showcase the pharmaceutical/ diagnostic implications of the nanotechnology approach. Manuscripts should aim, wherever possible, to demonstrate the in vivo impact of any nanotechnological intervention. As reducing a material to the nanoscale is capable of fundamentally altering the material’s properties, the journal’s readership is particularly interested in new characterisation techniques and the advanced properties that originate from this size reduction. Both bottom up and top down approaches to the realisation of nanomaterials lie within the scope of the journal.