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局部载双氯芬酸 Cubosomal 凝胶治疗白化病大鼠软组织损伤的潜力评估。

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

机构信息

I.T.S College of Pharmacy, Murad Nagar, Ghaziabad, Uttar Pradesh, India.

SRM Modinagar College of Pharmacy, SRM IST Delhi-NCR Campus, Modinagar, Uttar Pradesh, India.

出版信息

Assay Drug Dev Technol. 2022 Dec;20(8):367-376. doi: 10.1089/adt.2022.063.

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 . 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 parameters. The optimized cubosome formulation was chosen to develop cubosomal gel and evaluated for 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/cm 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.

摘要

肌肉拉伤是最常见的损伤之一,具有较高的间歇性发生率。由于拉伤损伤的多样性,不同的实验动物模型被用于研究具有可重复性结果的此类损伤。立方醇,一种新兴的纳米药物递送工具,被认为是脂溶性药物局部递送至治疗局部炎症的理想载体,可减少应用频率并延长作用时间。本工作描述了负载双氯芬酸的立方醇凝胶的研制,并研究了炎症和组织损伤的治疗。坐骨神经功能指数(SFI)是一种观察大鼠诱导损伤后后肢恢复的简单临床方法。首先,通过高压匀质法制备立方醇,并评价其参数。选择优化的立方醇配方来研制立方醇凝胶,并评价其体外参数,还研究了在大鼠胫骨前肌拉伤后 SFI 恢复的时间。立方醇配方(F4)表现出低的粒径(51.04±1.37nm)和低的多分散指数(0.085±1.13),以及负的zeta 电位(-32.8±0.67mV)。在大鼠中,与普通凝胶相比,立方醇凝胶制剂(CGF)的经皮渗透(402±6.08μg)和药物通量(15.71±0.82μg/cm h)有显著提高。此外,CGF 在 SFI 方面从第一天到第七天也有显著差异。大鼠皮肤的组织学显示,与阴性对照组相比,负载双氯芬酸的 CGF 治疗组有显著效果。

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