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辛伐他汀立方纳米载体的制备及评价及其促伤口愈合作用的评估。

Formulation and evaluation of simvastatin cubosomal nanoparticles for assessing its wound healing effect.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, 71526, Egypt.

Department of Pathology and Clinical Pathology, Faculty of Veterinary Medicine, Assiut University, Assiut, 71526, Egypt.

出版信息

Sci Rep. 2023 Oct 20;13(1):17941. doi: 10.1038/s41598-023-44304-2.

DOI:10.1038/s41598-023-44304-2
PMID:37864028
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10589326/
Abstract

Wound healing is one of the most challenging medical circumstances for patients. Pathogens can infect wounds, resulting in tissue damage, inflammation, and disruption of the healing process. Simvastatin was investigated recently, as a wound healing agent that may supersede the present therapies for wounds. Our goal in this paper is to focus on formulation of simvastatin cubosomes for topical delivery, as a potential approach to improve simvastatin skin permeation. By this technique its wound healing effect could be improved. Cubosomes were prepared using the top-down method and the prepared cubosomes were characterized by several techniques. The most optimal simvastatin cubosomal formulation was then included in a cubogel dosage form using different gelling agents. The results showed that the average particle size of the prepared cubosomes was 113.90 ± 0.58 nm, the entrapment efficiency was 93.95 ± 0.49% and a sustained simvastatin release was achieved. The optimized formula of simvastatin cubogel displayed pseudoplastic rheological behavior. This same formula achieved enhancement in drug permeation through excised rat skin compared to free simvastatin hydrogel with flux values of 46.18 ± 2.12 mcg cm h and 25.92 ± 3.45 mcg cm h respectively. Based on the in-vivo rat studies results, this study proved a promising potential of simvastatin cubosomes as wound healing remedy.

摘要

伤口愈合是患者面临的最具挑战性的医疗情况之一。病原体可能感染伤口,导致组织损伤、炎症和愈合过程中断。辛伐他汀最近被研究为一种伤口愈合剂,可能取代目前的伤口治疗方法。我们在本文中的目标是专注于辛伐他汀立方体制剂的局部递送来提高辛伐他汀的皮肤渗透。通过这种技术可以改善其伤口愈合效果。立方体制剂是通过自上而下的方法制备的,并通过多种技术对其进行了表征。然后将最优化的辛伐他汀立方体制剂包含在使用不同胶凝剂的立方凝胶剂型中。结果表明,所制备的立方体制剂的平均粒径为 113.90 ± 0.58nm,包封效率为 93.95 ± 0.49%,并实现了辛伐他汀的持续释放。辛伐他汀立方凝胶的优化配方表现出假塑性流变行为。与游离辛伐他汀水凝胶相比,该配方可显著提高药物透过离体大鼠皮肤的渗透,通量值分别为 46.18 ± 2.12mcg·cm-2·h-1和 25.92 ± 3.45mcg·cm-2·h-1。基于体内大鼠研究结果,本研究证明了辛伐他汀立方体制剂作为伤口愈合剂的有前途的潜力。

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