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首页> 外文期刊>Saudi Pharmaceutical Journal >Penetration enhancers in proniosomes as a new strategy for enhanced transdermal drug delivery
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Penetration enhancers in proniosomes as a new strategy for enhanced transdermal drug delivery

机译:proniosomes中的渗透促进剂作为增强透皮药物递送的新策略

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The aim of this work is to investigate penetration enhancers in proniosomes as a transdermal delivery system for nisoldipine. This was performed with the goal of optimising the composition of proniosomes as transdermal drug delivery systems. Plain proniosomes comprising sorbitan monostearate, cholesterol, ethanol and a small quantity of water were initially prepared. Subsequently, proniosomes containing lecithin or skin penetration enhancers were prepared and evaluated for transdermal delivery of nisoldipine. The plain proniosomes significantly enhanced the transdermal flux of nisoldipine to reach 12.18@mgcm^-^2h^-^1 compared with a saturated aqueous drug solution which delivered the drug at a rate of 0.46@mgcm^-^2h^-^1. Incorporation of lecithin into such proniosomes increased the drug flux to reach a value of 28.51@mgcm^-^2h^-^1. This increase can be attributed to the penetration enhancing effect of lecithin fatty acid components. Replacing lecithin oleic acid (OA) produced proniosomes of comparable efficacy to the lecithin containing system. The transdermal drug flux increased further after incorporation of propylene glycol into the OA based proniosomes. Similarly, incorporation of isopropyl myristate into plain proniosomes increased drug flux. The study introduced enhanced proniosomes as a promising transdermal delivery carrier and highlighted the role of penetration enhancing mechanisms in enhanced proniosomal skin delivery. The study opened the way for another line of optimisation of niosome proconcentrates.
机译:这项工作的目的是研究作为尼索地平的透皮给药系统的proniosomes中的渗透促进剂。这样做的目的是优化作为透皮药物递送系统的前体的组成。最初制备了包含脱水山梨糖醇单硬脂酸酯,胆固醇,乙醇和少量水的普通脂质体。随后,制备含有卵磷脂或皮肤渗透促进剂的原核小体并评估尼索地平的透皮递送。与以0.46@mgcm^-^2h^-^1的速率递送药物的饱和药物水溶液相比,普通的proniosomes大大提高了尼索地平的透皮通量,达到12.18@mgcm^-^2h^-^1。将卵磷脂掺入此类前体体中使药物通量增加至28.51mgmg ^-^ 2h ^-^ 1的值。这种增加可以归因于卵磷脂脂肪酸组分的渗透增强作用。替换卵磷脂油酸(OA)产生与含卵磷脂系统可比的功效的前体。在将丙二醇掺入基于OA的前体中后,透皮药物通量进一步增加。类似地,将肉豆蔻酸异丙酯掺入普通proniosome中会增加药物通量。这项研究介绍了增强的proniosomes作为有希望的透皮递送载体,并强调了渗透增强机制在增强proniosomal皮肤递送中的作用。该研究为进一步优化含脂质原液开辟了道路。

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