Influence of Orange Oil on Skin Permeability, Dermatokinetics, and In Vivo Anti-inflammatory Properties of Lornoxicam-loaded Niosomal Gel.

IF 1.8 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Narahari N Palei, Arghya K Dhar, Jayaraman Rajangam, Dharani Prasad P, Biswa Mohan Sahoo
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引用次数: 0

Abstract

Introduction: Lornoxicam is a non-steroidal anti-inflammatory drug belonging to the oxicam class. This study aimed to develop a niosomal gel containing orange oil for improving the anti-inflam-matory effect of lornoxicam.

Methods: Lornoxicam-loaded niosomes (LOR-OR-NIO) were prepared using film hydration followed by the sonication method. Particle size, entrapment efficiency, and ex vivo permeation were all consid-ered during the optimization of the niosomal gels by employing the Box-Behnken design. Dermatoki-netics and in vivo anti-inflammatory studies were performed using male Wistar rats.

Results: The particle size, entrapment efficiency, and skin permeation ability of the optimized LOR-OR-NIO formulation were found to be 354.3 nm, 83.56 %, and 105.63 μg/cm2, respectively. The ex vivo studies indicated that the optimized LOR-OR-NIO gel demonstrated superior drug penetration properties (105.43 μg/cm2) compared to both the LOR-NIO gel (69.23 μg/cm2) and the LOR gel (35.34 μg/cm2). The activation energy values of LOR gel, LOR-NIO gel, and LOR-OR-NIO gel were 2.74 Kcal mol-1, 1.93 Kcal mol-1, and 0.94 Kcal mol-1, respectively.

Discussion: The lower activation energy of the LOR-OR-NIO gel contributed to more skin penetration of the drug. Dermatokinetics investigation demonstrated that the LOR-OR-NIO gel had superior pene-tration in the epidermal and dermal areas compared to the LOR gel. In vivo anti-inflammatory studies indicated that the LOR-OR-NIO gel exhibited greater edema inhibition compared to both the LOR-NIO gel and LOR gel. These results demonstrated the enhanced anti-inflammatory activity of the LOR-OR-NIO gel.

Conclusion: The study concluded that orange oil enhanced skin permeability and influenced the derma-tokinetics of the LOR-OR-NIO gel, leading to an improvement in in vivo anti-inflammatory properties..

橙油对氯诺昔康乳质体凝胶皮肤通透性、皮肤动力学和体内抗炎特性的影响。
氯诺昔康是一种非甾体抗炎药,属于奥昔康类。本研究旨在研制一种含有橙油的乳质体凝胶,以提高氯诺昔康的抗炎作用。方法:采用膜水合-超声法制备氯诺昔康负载乳质体(lorno昔康- or - nio)。采用Box-Behnken设计优化乳质体凝胶时,考虑了颗粒大小、包裹效率和体外渗透。使用雄性Wistar大鼠进行皮肤动力学和体内抗炎研究。结果:优化后的LOR-OR-NIO配方的粒径为354.3 nm,包封率为83.56%,透皮能力为105.63 μg/cm2。离体实验表明,优化后的LOR- or - nio凝胶的药物渗透性能为105.43 μg/cm2,高于LOR- nio凝胶的69.23 μg/cm2和LOR凝胶的35.34 μg/cm2。LOR凝胶、LOR- nio凝胶和LOR- or - nio凝胶的活化能分别为2.74 Kcal mol-1、1.93 Kcal mol-1和0.94 Kcal mol-1。讨论:低活化能的LOR-OR-NIO凝胶有助于药物更多的皮肤渗透。皮肤动力学研究表明,与LOR凝胶相比,LOR- or - nio凝胶在表皮和真皮区域具有更好的渗透性。体内抗炎研究表明,与LOR- nio凝胶和LOR凝胶相比,LOR- or - nio凝胶具有更大的水肿抑制作用。这些结果表明,loro - or - nio凝胶具有增强的抗炎活性。结论:橙油可提高皮肤渗透性,影响凝胶的皮肤动力学,从而改善体内抗炎性能。
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来源期刊
Current drug metabolism
Current drug metabolism 医学-生化与分子生物学
CiteScore
4.30
自引率
4.30%
发文量
81
审稿时长
4-8 weeks
期刊介绍: Current Drug Metabolism aims to cover all the latest and outstanding developments in drug metabolism, pharmacokinetics, and drug disposition. The journal serves as an international forum for the publication of full-length/mini review, research articles and guest edited issues in drug metabolism. Current Drug Metabolism is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the most important developments. The journal covers the following general topic areas: pharmaceutics, pharmacokinetics, toxicology, and most importantly drug metabolism. More specifically, in vitro and in vivo drug metabolism of phase I and phase II enzymes or metabolic pathways; drug-drug interactions and enzyme kinetics; pharmacokinetics, pharmacokinetic-pharmacodynamic modeling, and toxicokinetics; interspecies differences in metabolism or pharmacokinetics, species scaling and extrapolations; drug transporters; target organ toxicity and interindividual variability in drug exposure-response; extrahepatic metabolism; bioactivation, reactive metabolites, and developments for the identification of drug metabolites. Preclinical and clinical reviews describing the drug metabolism and pharmacokinetics of marketed drugs or drug classes.
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