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壳聚糖包被脂质微泡包裹双氯芬酸对大鼠抗炎效果的评估

Assessment of the Anti-Inflammatory Effectiveness of Diclofenac Encapsulated in Chitosan-Coated Lipid Microvesicles in Rats.

作者信息

Pauna Ana-Maria Raluca, Tartau Liliana Mititelu, Vasilescu Alin Mihai, Abu Koush Angy, Stan Ruxandra Teodora, Moraru Marius Constatin, Popa Cosmin Gabriel, Gavril Liviu Ciprian, Florentina Gavril Roxana, Crauciuc Dragos Valentin, Radulescu Ana Marina, Stan Cristinel Ionel

机构信息

Department of Anatomy, Faculty of Medicine, "Grigore T. Popa" University of Medicine and Pharmacy, 700115 Iasi, Romania.

Department of Pharmacology, Faculty of Medicine, "Grigore T. Popa" University of Medicine and Pharmacy, 700115 Iasi, Romania.

出版信息

Pharmaceutics. 2025 May 3;17(5):607. doi: 10.3390/pharmaceutics17050607.

Abstract

: Diclofenac (DCF) is a widely used nonsteroidal anti-inflammatory drug (NSAID), but its conventional formulations may have limited efficacy and are associated with adverse effects. This study aimed to evaluate the anti-inflammatory and antioxidant effects of diclofenac encapsulated in chitosan-coated lipid microvesicles (DCF-m) compared to free DCF in a rat model of subacute inflammation. : DCF-m was prepared using L-α-phosphatidylcholine and coated with chitosan (CHIT). Subacute inflammation was induced using the cotton pellet granuloma model, and animals were divided into four groups ( = 5): a negative control group without granuloma receiving vehicle (double-distilled water), a control group with granuloma receiving vehicle, a group with granuloma treated with 15 mg/kg of free DCF, and a group with granuloma treated with 15 mg/kg of DCF-m. : Both DCF and DCF-m significantly reduced granuloma mass, body weight gain, and serum inflammatory markers compared to the control group with granuloma. Moreover, DCF-m treatment led to a more pronounced reduction in granulomatous inflammation and a greater enhancement of antioxidant enzyme activity than free DCF. : These findings suggest that DCF-m exhibits superior anti-inflammatory and antioxidant properties compared to conventional diclofenac in a model of subacute inflammation.

摘要

双氯芬酸(DCF)是一种广泛使用的非甾体抗炎药(NSAID),但其传统制剂的疗效可能有限且伴有不良反应。本研究旨在评估在亚急性炎症大鼠模型中,与游离双氯芬酸相比,壳聚糖包被脂质微泡包裹的双氯芬酸(DCF-m)的抗炎和抗氧化作用。:使用L-α-磷脂酰胆碱制备DCF-m并用壳聚糖(CHIT)包被。采用棉球肉芽肿模型诱导亚急性炎症,将动物分为四组(每组n = 5):无肉芽肿的阴性对照组给予赋形剂(双蒸水),有肉芽肿的对照组给予赋形剂,有肉芽肿的一组用15 mg/kg游离双氯芬酸治疗,有肉芽肿的一组用15 mg/kg DCF-m治疗。:与有肉芽肿的对照组相比,双氯芬酸和DCF-m均显著降低了肉芽肿质量、体重增加和血清炎症标志物。此外,与游离双氯芬酸相比,DCF-m治疗导致肉芽肿性炎症的减轻更明显,抗氧化酶活性的增强更大。:这些发现表明,在亚急性炎症模型中,与传统双氯芬酸相比,DCF-m具有更优越的抗炎和抗氧化特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d1/12115328/aaa214e5e543/pharmaceutics-17-00607-g001.jpg

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