Potential Assessment of Topical Felbinac-Loaded Cubosomal Gel in Soft Tissue Injury in Albino Rats.

IF 1.6 4区医学 Q4 BIOCHEMICAL RESEARCH METHODS

Assay and drug development technologies Pub Date : 2022-12-01 DOI:10.1089/adt.2022.063

Snigdha Bhardwaj, Anshul, Praveen Kumar Gaur, Sonam Bhatia

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Abstract

Muscle strain is one of the most common injuries with high intermittence rate. Due to diverseness of strain injuries, different experimental animal models are employed to investigate such injuries with reproducible results. Cubosomes, an emerging nano drug delivery tool, are considered ideal carriers for the topical delivery of lipophilic drugs to treat local inflammations with reduced frequency of application for prolonged periods. This work describes the development of Felbinac-loaded cubosomal gel and investigated the treatment of inflammation and tissue injury in vivo. Sciatic Function Index (SFI) is a simple clinical method to observe hind limb recovery in rats after induced injuries. First, cubosomes were fabricated by high-pressure homogenization process and evaluated for in vitro parameters. The optimized cubosome formulation was chosen to develop cubosomal gel and evaluated for in vitro parameters and also investigated time to recovery of SFI after strain induction in tibialis anterior muscles in rats. The cubosome formulation (F4) exhibited low droplet size (51.04 ± 1.37 nm)and polydispersity index (0.085 ± 1.13), and negative zeta potential (-32.8 ± 0.67 mV). In rats, topical application of cubosomal gel formulation (CGF) exhibited significant improvement in skin permeation (402 ± 6.08 μg) and drug flux (15.71 ± 0.82 μg/cm² h) compared to plain gel. Also, CGF demonstrated significant difference in SFI from first to seventh day. The histology of rat skin showed significant effect for groups treated with Felbinac-loaded CGF compared to a negative control group.

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外用负载felbinac的立方体凝胶治疗白化大鼠软组织损伤的潜力评估。

肌肉拉伤是最常见的间歇性损伤之一。由于应变损伤的多样性，采用不同的实验动物模型来研究应变损伤，结果具有可重复性。立方体体是一种新兴的纳米药物递送工具，被认为是局部递送亲脂性药物的理想载体，可以减少长时间应用的频率，治疗局部炎症。本研究描述了负载felbinac的立方体凝胶的发展，并研究了体内炎症和组织损伤的治疗。坐骨功能指数(SFI)是观察大鼠后肢损伤后恢复情况的一种简便的临床方法。首先，采用高压均质工艺制备了立方体体，并对其体外参数进行了评价。选择优化后的立方体配方制备立方体凝胶，评估其体外参数，并研究大鼠胫骨前肌应变诱导后SFI的恢复时间。该长方体配方(F4)具有低液滴尺寸(51.04±1.37 nm)和多分散性指数(0.085±1.13)和负zeta电位(-32.8±0.67 mV)的特点。在大鼠中，与普通凝胶相比，局部应用立方体凝胶制剂(CGF)可显著改善皮肤渗透(402±6.08 μg)和药物通量(15.71±0.82 μg/cm2 h)。此外，CGF在第1天和第7天的SFI表现出显著差异。与阴性对照组相比，含felbinac的CGF组对大鼠皮肤组织学有显著影响。

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

Assay and drug development technologies 医学-生化研究方法

CiteScore

3.60

自引率

0.00%

发文量

审稿时长

>12 weeks

期刊介绍： ASSAY and Drug Development Technologies provides access to novel techniques and robust tools that enable critical advances in early-stage screening. This research published in the Journal leads to important therapeutics and platforms for drug discovery and development. This reputable peer-reviewed journal features original papers application-oriented technology reviews, topical issues on novel and burgeoning areas of research, and reports in methodology and technology application. ASSAY and Drug Development Technologies coverage includes: -Assay design, target development, and high-throughput technologies- Hit to Lead optimization and medicinal chemistry through preclinical candidate selection- Lab automation, sample management, bioinformatics, data mining, virtual screening, and data analysis- Approaches to assays configured for gene families, inherited, and infectious diseases- Assays and strategies for adapting model organisms to drug discovery- The use of stem cells as models of disease- Translation of phenotypic outputs to target identification- Exploration and mechanistic studies of the technical basis for assay and screening artifacts