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用于增强氯诺昔康经皮递送的脂质体凝胶制剂:体外和体内评价

Formulation of Niosomal Gel for Enhanced Transdermal Lornoxicam Delivery: In-Vitro and In-Vivo Evaluation.

作者信息

El-Ridy Mohamed Shafik, Yehia Soad Aly, Mohsen Amira Mohamed, El-Awdan Sally A, Darwish Asmaa Badawy

机构信息

Pharmaceutical Technology Department, National Research Centre, Dokki, Cairo. Egypt.

Pharmaceutics Department, Faculty of Pharmacy, Cairo University, Cairo. Egypt.

出版信息

Curr Drug Deliv. 2018;15(1):122-133. doi: 10.2174/1567201814666170224141548.

Abstract

BACKGROUND

The objective of this study was to investigate the potential of niosomal gels as a transdermal delivery system to improve the permeation and anti-inflammatory activity of Lornoxicam (LX).

METHODS

LX niosomes were prepared by thin film hydration technique and were characterized using Transmission Electron Microscopy (TEM), Differential Scanning Calorimetry (DSC), Particle Size analysis and Zeta potential determination. LX niosomal gel/LX loaded gel were prepared using Carbopol 934 (2%) and were evaluated for their physical appearance, pH and rheological behaviour. Ex vivo skin permeation test was performed on dorsal region of wistar rats. In vivo studies comprised skin irritation test and anti-inflammatory activity study.

RESULTS

The prepared LX niosomes exhibited an entrapment efficiency of more than 66% and a particle size diameter ranging from 295 nm to 1298 nm, with negatively charged zeta potential. TEM electron micrographs revealed spherical shaped vesicles. The release pattern of drug was analyzed and found to follow Higuchi's model. Rheology studies revealed the pseudoplastic behaviour of LX niosomal gel. They exhibited a one and half fold increase in drug permeated through rat skin, when compared to free drug. Skin irritation test proved the non-irritancy of LX niosomal gels, when applied to dorsal region of Wistar rats. Percentage edema inhibition of LX niosomes was significantly higher (P<0.05) than that of free LX group showing an enhanced anti-inflammatory activity of LX niosomes.

CONCLUSION

These findings revealed that LX loaded niosomal gels could be a potential transdermal drug delivery system.

摘要

背景

本研究的目的是探究非离子表面活性剂囊泡凝胶作为透皮给药系统提高氯诺昔康(LX)渗透和抗炎活性的潜力。

方法

采用薄膜水化技术制备LX非离子表面活性剂囊泡,并用透射电子显微镜(TEM)、差示扫描量热法(DSC)、粒度分析和zeta电位测定对其进行表征。使用卡波姆934(2%)制备LX非离子表面活性剂囊泡凝胶/LX负载凝胶,并对其外观、pH值和流变行为进行评估。在Wistar大鼠背部进行离体皮肤渗透试验。体内研究包括皮肤刺激性试验和抗炎活性研究。

结果

制备的LX非离子表面活性剂囊泡包封率超过66%,粒径范围为295nm至1298nm,zeta电位为负。TEM电子显微镜照片显示为球形囊泡。分析药物释放模式,发现其符合Higuchi模型。流变学研究表明LX非离子表面活性剂囊泡凝胶具有假塑性行为。与游离药物相比,它们在大鼠皮肤中的药物渗透率提高了1.5倍。皮肤刺激性试验证明,将LX非离子表面活性剂囊泡凝胶应用于Wistar大鼠背部时无刺激性。LX非离子表面活性剂囊泡的水肿抑制百分比显著高于游离LX组(P<0.05),表明LX非离子表面活性剂囊泡具有增强的抗炎活性。

结论

这些发现表明,负载LX的非离子表面活性剂囊泡凝胶可能是一种潜在的透皮给药系统。

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