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Effects of Sting Plant Extracts as Penetration Enhancers on Transdermal Delivery of Hypoglycemic Compounds

机译:刺植物提取物作为渗透促进剂对降血糖化合物透皮递送的影响

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摘要

Background and objectives: The percutaneous route is an interesting and inventive investigation field of drug delivery. However, it is challenging for drug molecules to pass through the skins surface, which is a characterized by its permeability barrier. The purpose of this study is to look at the effect of some penetration enhancers on in vivo permeation of insulin and insulin sensitizers (curcumin and rutin) through diabetes-induced mouse skin. Materials and Methods: Sting crude extracts of Dendrocnide meyeniana, Urtica thunbergiana Sieb. and Zucc, and Alocasia odora (Lodd.) Spach were used as the penetration enhancers. Mouse skin irritation was tested by smearing the enhancers for the measurements at different time points and the cell viability of the HaCaT human skin keratinocytes, which was determined by Trypan blue exclusion and MTT assays to evaluate human biosafety for these extracts after the mouse skin permeation experiments. Results: All enhancers induced a slight erythema without edema on the mouse skin that completely recovered after 6 h from the enhancer smears as compared with normal mouse skin. Furthermore, no damaged cells were found in the HaCaT keratinocytes under sting crude extract treatments. The blood sugar level in the diabetic mice treated with the insulin or insulin sensitizers, decreased significantly (p < 0.05) in the presence of enhancers. The area under the curve (AUC) values of transdermal drug delivery (TDD) ranged from 42,000 ± 5000 mg/dL x min without enhancers, to 30,000 ± 2000 mg/dL x min in the presence of enhancers. Conclusions: This study exhibited that natural plant extracts could be preferred over the chemically synthesized molecules and are safe and potent penetration enhancers for stimulating the transdermal absorption of drugs.
机译:背景和目的:经皮途径是药物输送的一个有趣的发明领域。然而,药物分子穿过皮肤表面具有挑战性,其特征在于其渗透性屏障。这项研究的目的是研究某些渗透促进剂对通过糖尿病引起的小鼠皮肤对胰岛素和胰岛素敏化剂(姜黄素和芦丁)的体内渗透的影响。材料和方法:刺取的树毛粗提物,黑叶荨麻。和Zucc,以及海芋(Loloc。Spach)用作渗透促进剂。通过在不同时间点涂增强剂以测量HaCaT人皮肤角质形成细胞的细胞活力和HaCaT人皮肤角质形成细胞的细胞活力来测试小鼠的皮肤刺激性,这是通过台盼蓝排除法和MTT试验确定的,以评估小鼠皮肤渗透实验后这些提取物的人生物安全性。结果:与正常小鼠皮肤相比,所有增强剂在小鼠皮肤上均引起轻微的红斑,而没有水肿,从增强剂涂片上涂药6小时后完全恢复。此外,经粗提取物处理后,HaCaT角质形成细胞中未发现受损细胞。在存在增强剂的情况下,用胰岛素或胰岛素增敏剂治疗的糖尿病小鼠的血糖水平显着降低(p <0.05)。在没有增强剂的情况下,透皮给药(TDD)的曲线下面积(AUC)值范围为42,000±5000 mg / dL x min,在存在增强剂的情况下为30,000±2000 mg / dL x min。结论:这项研究表明,天然植物提取物可能比化学合成分子更可取,并且是安全有效的渗透促进剂,可刺激药物的透皮吸收。

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