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载克霉唑电纺纳米纤维两种不同方法药物释放的比较研究:全自动化顺序注射系统的应用。

Comparative study of drug release from electrospun nanofibers loaded with clotrimazole via two different approaches using a fully automated sequential injection system.

机构信息

Department of Analytical Chemistry, Faculty of Pharmacy in Hradec Králové, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.

Department of Analytical Chemistry, Faculty of Pharmacy in Hradec Králové, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic; Faculty of Drug Sciences, University of Milan, Via Festa Del Perdono 7, 20122 Milano Italy.

出版信息

Talanta. 2024 Mar 1;269:125415. doi: 10.1016/j.talanta.2023.125415. Epub 2023 Nov 21.

Abstract

The development of new drug delivery platforms including the use of nanotechnology has been found of great interest in recent years. Two different loading approaches of the model antimycotic drug clotrimazole into the nanofibrous polycaprolactone and polydioxanone structures including electrospinning of a drug-polymer blend and impregnation of nanofibers with drug have been tested. The final amount of clotrimazole in the nanofibrous materials was determined by HPLC analysis and Raman spectroscopy. The electrospinning of blend approach allowed the adsorption of clotrimazole in a quantity of up to 30 % using mixtures with polymer/clotrimazole ratios from 2:1 to 8:1 (w/w). Ethanolic clotrimazole solutions with concentrations from 2.5 to 3.5 mg L were used for adsorbing clotrimazole in blank nanofibers for 1-3 h with final clotrimazole content ranging from 3.0 to 5.7 %. Furthermore, a comparative liberation study including comparison with commercially available creams was carried out in low pressure flow system. The results obtained confirmed well controlled release of clotrimazole from both types of nanofibers. Compared to commercial pharmaceutical formulations containing 1 % clotrimazole where first-order release kinetics was observed, nanofibrous materials provided linear controlled release (zero-order kinetics) in the tested 3 h period.

摘要

近年来,包括纳米技术在内的新型药物输送平台的发展引起了极大的关注。本文测试了两种不同的载药方法,即将模型抗真菌药物克霉唑载入到纳米纤维聚己内酯和聚二氧杂环己酮结构中,包括药物-聚合物共混物的静电纺丝和纳米纤维的药物浸渍。通过 HPLC 分析和拉曼光谱法确定了纳米纤维材料中克霉唑的最终含量。共混物静电纺丝方法允许使用聚合物/克霉唑比例为 2:1 至 8:1(w/w)的混合物吸附多达 30%的克霉唑。使用浓度为 2.5 至 3.5 mg L 的克霉唑乙醇溶液,在空白纳米纤维中吸附克霉唑 1-3 小时,最终克霉唑含量在 3.0 至 5.7%之间。此外,还进行了包括与市售乳膏比较的低压流动系统的比较释放研究。所得结果证实了两种类型的纳米纤维均能很好地控制克霉唑的释放。与含有 1%克霉唑的市售药物制剂相比,观察到的是一级释放动力学,而纳米纤维材料在测试的 3 小时内提供了线性控制释放(零级动力学)。

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