Liquid Crystal Nanoparticles-based Fluocinolone Acetonide Topical Gel for Atopic Dermatitis: In vitro and in vivo Study

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2024-04-17 DOI:10.1007/s12247-024-09829-7
Chaitanya Shirke, Sarika Wairkar
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Abstract

Purpose

Fluocinolone acetonide is a potent anti-inflammatory corticosteroid commonly used to treat atopic dermatitis. Its commercially available topical formulations (cream/ointment) must be administered frequently. The study aimed to develop a fluocinolone acetonide-liquid crystal nanoparticles (FA-LCN) based gel for treating atopic dermatitis.

Methods

FA-LCN were produced using a top-down method and statistically optimized by a 23 full-factorial design with concentrations of glyceryl monooleate, Poloxamer 407 and sonication time as independent variables, while entrapment efficacy (EE), particle size (PS) and in vitro drug release (DR) as dependent variables.

Results

The optimized batch with an average particle size of 265.3 nm, zeta potential of -47.3 mV and encapsulation efficiency of 98.6% was incorporated into Carbopol 940-based gel. The globular nanoparticles were confirmed by TEM analysis, and their formation was supported by FTIR data. In vitro studies of FA-LCN gel showed 96 ± 1.65% release at the end of 30 h. In vivo studies revealed no skin irritation after the application of FA-LCN gel. FA-LCN (0.5%w/w) gel showed faster healing, substantially reduced earflap thickness, and lower WBC counts compared to the FA-LCN 0.1% gel and the marketed formulation in albino Wistar rats challenged with DNCB. Additionally, the FA-LCN 0.5% gel (3.08 ± 0.16 µg/cm2) exhibited greater drug deposition in the skin compared to the FA-LCN 0.1% (2.12 ± 0.11 µg/cm2) gel and the marketed formulation (1.01 ± 0.19 µg/cm2).

Conclusions

Therefore, FA-LCN-based gel could be a viable option for chronic dermatological treatment for atopic dermatitis with a reduced application frequency.

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用于特应性皮炎的液晶纳米颗粒氟西诺龙-阿塞通内酯外用凝胶:体外和体内研究
目的氟西诺龙丙酮是一种强效消炎皮质类固醇,常用于治疗特应性皮炎。其市售外用制剂(霜剂/膏剂)必须频繁使用。该研究旨在开发一种基于氟西诺龙-丙酮液晶纳米颗粒(FA-LCN)的凝胶,用于治疗特应性皮炎。方法采用自上而下的方法生产 FA-LCN,并通过 23 全因子设计进行统计优化,以甘油单油酸酯、Poloxamer 407 的浓度和超声时间为自变量,以夹持效力(EE)、粒度(PS)和体外药物释放(DR)为因变量。结果将平均粒径为265.3 nm、zeta电位为-47.3 mV、包封效率为98.6%的优化批次纳入Carbopol 940凝胶中。球状纳米颗粒经 TEM 分析证实,其形成得到了傅立叶变换红外光谱数据的支持。体外研究显示,FA-LCN凝胶在30小时后的释放量为96 ± 1.65%。与 FA-LCN 0.1%凝胶和市场上销售的配方相比,FA-LCN(0.5%w/w)凝胶在白化 Wistar 大鼠的 DNCB 治疗中显示出更快的愈合速度、大幅减少的耳瓣厚度和更低的白细胞计数。此外,与 FA-LCN 0.1%凝胶(2.12 ± 0.11 µg/cm2)和市售配方(1.01 ± 0.19 µg/cm2)相比,FA-LCN 0.5%凝胶(3.08 ± 0.16 µg/cm2)在皮肤中的药物沉积更多。
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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
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.
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