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首页> 外文期刊>Biomedicine & pharmacotherapy =: Biomedecine & pharmacotherapie >Formulation and optimization of lacidipine loaded niosomal gel for transdermal delivery: In-vitro characterization and in-vivo activity
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Formulation and optimization of lacidipine loaded niosomal gel for transdermal delivery: In-vitro characterization and in-vivo activity

机译:用于透皮递送的LACIDIPIN LACIDIPIN LACIPIPIN LACIPIPIN LACIDIPIN的憩室凝胶的制剂和优化:体外表征和体内活性

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摘要

The aim of the present research work is to formulate lacidipine (LAC) loaded niosomes formulation for the management of hypertension by thin film hydration technique. The developed formulations were statistically optimized by four factors, three levels Box-Behnken design and were evaluated for vesicle size, entrapment efficiency, and flux. The optimized LAC niosomes was further evaluated for permeation depth by confocal laser scanning microscopy (CLSM) and converted to gel formulation. Further, the optimized LAC niosomes gel was evaluated for ex-vivo permeation study, skin irritation study, stability study and pharmacodynamics study. The optimized LAC niosomes formulation showed vesicle size, entrapment efficiency and flux value of 676.98 +/- 10.92 nm, 82.77 +/- 4.34% and 38.43 +/- 2.43 mu g/cm(2)/h respectively, with spherical morphology. The comparative CLSM study showed that optimized LAC niosomes formulation has shown maximum permeation (70.75 mu m) as compare to LAC liposomes formulation (58.26 mu m). The optimized LAC niosomes gel showed skin permeation enhancement of 2.15 times as compare to control gel. Furthermore, in vivo antihypertensive activity showed significantly higher (p < 0.001) reduction in blood pressure compared to oral suspension. Indeed, it was found that niosomal vesicles represented to be an efficient nano vesicular carrier for transdermal delivery of lacidipine. (C) 2017 Published by Elsevier Masson SAS.
机译:目前研究工作的目的是通过薄膜水合作技术制备曲叶饼(LAC)加载的定期组合物,用于管理高血压的管理。开发的配方通过四个因素进行了统计优化,三级Box-Behnken设计,并评估了囊泡尺寸,截留效率和助焊剂。通过共聚焦激光扫描显微镜(CLSM)进一步评估优化的曲线肌瘤,得到渗透深度并转化为凝胶制剂。此外,评估了优化的Lac Niosomes凝胶,用于前体内渗透研究,皮肤刺激研究,稳定性研究和药效学研究。优化的曲线定位体配方显示囊泡尺寸,夹带效率和通量值,分别为676.98 +/- 10.92nm,82.77 +/- 4.34%和38.43 +/-2.43μg/ cm(2)/ h,具有球形形态。比较CLSM研究表明,优化的曲线肌瘤配方表明,与脂质体配方(58.26μm)相比,最大渗透(70.75μm)。优化的Lac Niosomes凝胶显示皮肤渗透增强2.15倍,与控制凝胶相比。此外,与口服悬浮液相比,体内抗高血压活性显着降低(P <0.001)血压降低。实际上,发现具有用于脱皮素递送的透皮递送的有效纳米囊泡载体的憩室囊泡。 (c)2017年由elestvier Masson SA发布。

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