他沙罗汀纳米凝胶外用治疗切除伤口的研究进展

Shanta Mahajan, Kirandeep Kaur, N. Saini, T. Chaudhary, Lovedeep Nim, Neena Bedi
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引用次数: 0

摘要

本研究的目的是开发和评估他扎罗汀的局部纳米乳液制剂,用于有效治疗切除伤口。塔扎罗汀(TZR)是一种用于治疗痤疮和银屑病的类视黄醇衍生物,最近的研究表明其具有良好的伤口愈合潜力。尽管它具有巨大的伤口愈合潜力,但它存在低水溶性和局部生物利用度的药代动力学限制。据报道,TZR的常规市售制剂在局部应用后会引起严重的皮肤刺激和发红。有鉴于此,本研究旨在开发基于纳米乳液的凝胶,以解决上述药代动力学和药效学问题。该研究的目的是开发一种稳定有效的负载他扎罗汀的纳米乳胶凝胶,用于治疗切除伤口,也可以克服与天然药物相关的问题。根据其对他扎罗汀的增溶潜力,选择了各种油、表面活性剂和助表面活性剂。构建了假三元相图,以获得不同比例的油、表面活性剂:共表面活性剂(Smix)和水的稳定纳米乳液区域,并确定他扎罗汀稳健配方的最佳浓度范围。研究了各种表征参数,以研究具有所需性质的纳米乳液的优化配方。进行了还原力分析和阶段性研究,以确定所开发的纳米乳胶凝胶的伤口愈合潜力。以茶树油为原料,以吐温20为表面活性剂,PEG400为共表面活性剂成功制备了TZR负载纳米乳液。所制备的纳米乳液是热力学稳定的,并且使用Carbopol 940作为可生物降解的胶凝聚合物进一步胶凝。制备的凝胶具有良好的铺展性、药物渗透性和稳定性。体内研究表明,优化配方成功掩盖了他扎罗汀的刺激性。此外,与对照组相比,所开发的纳米乳液凝胶的药效学评估显示,除了显著的伤口收缩外,还具有显著的镇痛和抗炎特性。结果表明,与市场上的配方相比,所开发的纳米乳液有潜力克服发红和红斑等缺点。与其他药物相比,它也显示出显著的治疗效果
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Development and Evaluation of Topical Nanoemulgel Formulation of Tazarotene for Effective Treatment of Excision Wounds
The aim of the present investigation entails the development and evaluation of topical nanoemulgel formulation of tazarotene for effective treatment of excision wounds Tazarotene (TZR) is a retinoid derivative marketed for the treatment of acne and psoriasis and the recent investigations indicate its excellent wound healing potential. Despite having magnificent wound healing potential, it suffers from pharmacokinetic limitations of low aqueous solubility and local bioavailability. Conventional marketed formulations of TZR have been reported to cause significant skin irritation and redness after its topical application. Keeping this in view, present investigation was designed to develop nanoemulsion based gel with intention to resolve the above mentioned pharmacokinetic and pharmacodynamic issues. The goal of the study was to develop a stable and effective tazarotene-loaded nanoemulgel for treating excision wounds which can also overcome the issues associated with the native drug. Various oils, surfactants and co-surfactants were selected on the basis of their solubilisation potential for tazarotene. Pseudoternary phase plots were constructed to obtain stable nanoemulsion region for various proportions of oil, surfactant: co-surfactant (Smix) and water and determine optimized concentration ranges for robust formulation of tazarotene. Various characterization parameters were studied to investigate the optimized formulation having desired attributes of nanoemulsion. Reducing power assay and phamacodymanic studies were conducted to determine the wound healing potential of developed nanoemulgel. TZR loaded nanoemulsion was successfully developed with nano-sized globules using tea tree oil with Tween 20 as surfactant and PEG 400 as co-surfactant. Prepared nanoemulsions were thermodynamically stable and were further gellified using Carbopol 940 as biodegradable gelling polymer. Prepared gels showed good spreadability, drug permeation and stability. In vivo investigations demonstrated that optimized formulation successfully masked the irritant nature of tazarotene. Moreover, the pharmacodynamic evaluation of developed nanoemulsion gel revealed its significant analgesic, anti-inflammatory properties in addition to its markable wound contraction as compared to control. The results demonstrated potential of developed nanoemulgel over marketed formulation to overcome the drawbacks like redness and erythema. It also showed significant healing efficacy over other
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来源期刊
Current Nanomedicine
Current Nanomedicine Medicine-Medicine (miscellaneous)
CiteScore
2.00
自引率
0.00%
发文量
15
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