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联合纳米载体和硅制微针应用提高酮洛芬经皮传递。

Improved percutaneous delivery of ketoprofen using combined application of nanocarriers and silicon microneedles.

机构信息

School of Pharmacy, University College Cork, Cork, UK; Department of Pharmacy, Faculty of Medicine, University of Banja Luka, Banja Luka, Bosnia and Herzegovina.

出版信息

J Pharm Pharmacol. 2013 Oct;65(10):1451-62. doi: 10.1111/jphp.12118. Epub 2013 Aug 5.

Abstract

OBJECTIVES

The aim of our study was to evaluate the effect of designing ketoprofen-loaded nanosized spheres and combining them with solid silicon microneedles for enhanced and sustained percutaneous drug delivery.

METHODS

Ketoprofen-loaded nanoparticles (KET-NP) were designed by modified solvent displacement method, using poly (D, L-lactic acid) (PDLLA). All prepared nanoparticles were characterised with regard to their particle size distribution, morphology, surface properties, thermal behaviour, drug content, drug release and stability. In-vitro skin permeation studies were conducted on Franz-type diffusion cells using porcine skin treated with ImmuPatch silicon microneedles (Tyndall Nation Institute, Cork, Ireland).

KEY FINDINGS

The study showed that uniform nanospheres were prepared with high encapsulation efficiency and retained stable for 2 months. After an initial burst release, the PDLLA nanoparticles were capable of sustaining and controlling ketoprofen release that followed Korsmeyer-Peppas kinetics. An enhanced flux of ketoprofen was observed in the skin treated with silicon microneedles over a prolonged period of time.

CONCLUSIONS

Following application of silicon microneedle arrays, KET-NP were able to enhance ketoprofen flux and supply the porcine skin with drug over a prolonged (24 h) period of time. Our findings indicate that the delivery strategy described here could be used for the further development of effective and painless administration systems for sustained percutaneous delivery of ketoprofen.

摘要

目的

我们的研究旨在评估设计载有酮洛芬的纳米球并将其与固体硅微针结合以增强和持续经皮药物传递的效果。

方法

使用聚(D,L-丙交酯)(PDLLA)通过改良的溶剂置换法设计载有酮洛芬的纳米颗粒(KET-NP)。所有制备的纳米颗粒均通过粒径分布、形态、表面性能、热行为、药物含量、药物释放和稳定性进行了表征。使用 ImmuPatch 硅微针(爱尔兰科克郡的 Tyndall 国家研究所)处理的猪皮,在 Franz 型扩散池上进行了体外皮肤渗透研究。

主要发现

研究表明,制备了具有高包封效率且稳定 2 个月的均匀纳米球。在初始突释后,PDLLA 纳米球能够持续控制酮洛芬释放,符合 Korsmeyer-Peppas 动力学。在长时间内,硅微针处理的皮肤中观察到酮洛芬通量增加。

结论

硅微针阵列应用后,KET-NP 能够增强酮洛芬通量,并在延长(24 小时)的时间内向猪皮提供药物。我们的研究结果表明,这里描述的传递策略可用于进一步开发有效且无痛的酮洛芬持续经皮传递的给药系统。

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