Skin delivery of nisoldipine from niosome proconcentrate

Article history: Received on: 07/11/2013 Revised on: 21/12/2013 Accepted on: 16/01/2014 Available online: 27/02/2014 Nisoldipine is used for treatment of hypertension and angina pectoris. However, it suffers from very low bioavailability due to its extensive pre-systemic metabolism. This together with its low dose made it excellent candidate for transdermal delivery. Accordingly, the aim of this study was to develop and evaluate transdermal delivery system for optimization of nisoldipine skin permeability. Proniosomes comprising cholesterol and span 60 with different ratios together with ethanol and minimal water were evaluated for such aim. The developed formulations were assessed with respect to drug entrapment efficiency, viscosity, in vitro drug release and transdermal permeability. All proniosomal formulations have significantly enhanced transdermal delivery of nisoldipine compared with saturated aqueous solution of the drug. Increasing cholesterol content resulted in reduced drug flux. The study was extended to compare the efficacy of such proniosomes to the corresponding niosomes. Proniosomes significantly optimized transdermal delivery of nisoldipine compared to their hydrated form. Such results contradict the hypothesis which claimed the necessity for niosome formation from proniosomes for efficient transdermal delivery with penetration enhancement being mainly responsible for improved delivery.

文章历史记录：收到：2013年7月11日修订：21/12/2013接受：16/01/2014在线提供：27/02/2014 Nisoldipine用于治疗高血压和心绞痛。但是，由于其广泛的系统前代谢，它的生物利用度非常低。这及其低剂量使其成为透皮递送的绝佳候选者。因此，这项研究的目的是开发和评估透皮递送系统，以优化尼索地平皮肤渗透性。以这种目的评估了包含胆固醇和乙醇和最小水的不同比例的胆固醇和60个跨度60。根据药物夹带效率，粘度，体外药物释放和透皮渗透性评估了开发的制剂。与该药物的饱和水溶液相比，所有肾小球制剂均显着增强了Nisoldipine的透皮递送。胆固醇含量的增加导致药物通量减少。扩展了该研究以比较此类proniosom体的功效与相应的Nioosomes。与水合形式相比，肾小腺体可以显着优化了尼索地平的透皮递送。这样的结果与假设相矛盾，该假设声称有必要从prio虫组体形成有效的透皮递送，而穿透性增强主要负责改善递送。