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首页> 外文期刊>Life sciences >Development and characterization of a novel controlled release drug delivery system based on nanostructured lipid carriers gel for meloxicam
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Development and characterization of a novel controlled release drug delivery system based on nanostructured lipid carriers gel for meloxicam

机译：基于纳米结构脂质载体凝胶的美洛昔康新型控释给药系统的研制与表征

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Aim: The main objective of the current investigation was to develop nanostructured lipid carriers (NLC) based gel for the enhancement of transdermal absorption of meloxicam (MLX) to achieve local as well as systemic drug action without concurrent gastrointestinal toxicity. Main methods: NLC gel containing MLX was prepared and characterized for particle size, polydispersity, zeta potential, pH, rheology, entrapment efficiency, occlusion factor, and thermal behavior. In vitro drug release, in vitro skin permeation and deposition studies were carried out using Franz diffusion cells. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) of MLX-NLC gel treated stratum corneum (SC) were undertaken to get an insight into the skin permeation enhancement mechanism of MLX-NLC gel. Toxicity potential of the developed gel formulation was assessed by in vitro hemolysis and histopathological examinations. The rat paw edema test was performed to evaluate the anti-inflammatory activity of MLX-NLC gel. Key findings: MLX-NLC gel demonstrated sustained release and enhanced the skin permeation and deposition of meloxicam especially into the dermis in comparison to meloxicam gel (control). MLX-NLC had an impact on the barrier properties of the skin and acted via protein and lipid modifications in the stratum corneum. MLX-NLC gel turned out to be hemocompatible, non-irritant, and non toxic with significant anti-inflammatory activity. Significance: The results suggest that NLC gel could be a promising carrier for the transdermal delivery of meloxicam.
机译：目的：当前研究的主要目的是开发基于纳米结构脂质载体（NLC）的凝胶，以增强美洛昔康（MLX）的透皮吸收，从而实现局部和全身性药物作用，而不会同时引起胃肠道毒性。主要方法：制备了含MLX的NLC凝胶，并对其粒径，多分散性，ζ电位，pH，流变性，包封率，吸留系数和热行为进行了表征。使用Franz扩散池进行了体外药物释放，体外皮肤渗透和沉积研究。进行了MLX-NLC凝胶处理的角质层（SC）的差示扫描量热法（DSC）和傅里叶变换红外光谱（FTIR），以深入了解MLX-NLC凝胶的皮肤渗透增强机理。通过体外溶血和组织病理学检查评估了所开发凝胶制剂的毒性潜力。进行大鼠爪水肿测试以评估MLX-NLC凝胶的抗炎活性。关键发现：与美洛昔康凝胶（对照）相比，MLX-NLC凝胶表现出缓释作用，并增强了美洛昔康的皮肤渗透和沉积，特别是进入真皮层。 MLX-NLC对皮肤的屏障特性有影响，并通过角质层中的蛋白质和脂质修饰起作用。 MLX-NLC凝胶具有血液相容性，无刺激性和无毒且具有显着的抗炎活性。启示：该结果表明NLC凝胶可能是美洛昔康透皮给药的一种有希望的载体。

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