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通过静电纺丝制备的乙酰唑胺眼内植入物的形态学和释放曲线的比较分析

Comparative Analysis of Morphological and Release Profiles in Ocular Implants of Acetazolamide Prepared by Electrospinning.

作者信息

Morais Mariana, Coimbra Patrícia, Pina Maria Eugénia

机构信息

Faculty of Pharmacy of University Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.

Department of Chemical Engineering, University Coimbra, CIEPQPF, Rua Sílvio Lima, Pólo II-Pinhal de Marrocos, 3030-790 Coimbra, Portugal.

出版信息

Pharmaceutics. 2021 Feb 15;13(2):260. doi: 10.3390/pharmaceutics13020260.

Abstract

The visual impairment that often leads to blindness causes a higher morbidity rate. The goal of this work is to create a novel biodegradable polymeric implant obtained from coaxial fibers containing the dispersed drug-acetazolamide-in order to achieve sustained drug release and increase patient compliance, which is of the highest importance. Firstly, during this work, uncoated implants were produced by electrospinning, and rolled in the shape of small cylinders that were composed of uniaxial and coaxial fibers with immobilized drug inside. The fibers were composed by PCL (poly ε-caprolactone) and Lutrol F127 (poly (oxyethylene-b-oxypropylene-b-oxyethylene)). The prepared implants exhibited a fast rate of drug release, which led to the preparation of new implants incorporating the same formulation but with an additional coating film prepared by solvent casting and comprising PCL and Lutrol F127 or PCL and Luwax EVA 3 ((poly (ethylene-co-vinyl acetate)). Implants were characterized and in vitro release profiles of acetazolamide were obtained in phosphate buffered saline (PBS) at 37 °C. The release profile of the acetazolamide from coated implant containing Luwax EVA 3 is considerably slower than what was observed in case of coated implants containing Lutrol F127, allowing a sustained release and an innovation relatively to other ocular drug delivery systems.

摘要

常导致失明的视力障碍会引发更高的发病率。这项工作的目标是制造一种新型的可生物降解聚合物植入物,该植入物由含有分散药物乙酰唑胺的同轴纤维制成,以实现药物的持续释放并提高患者的依从性,这是至关重要的。首先,在这项工作中,通过静电纺丝制备未涂层的植入物,并将其卷成小圆柱体形状,这些小圆柱体由单轴和同轴纤维组成,内部固定有药物。纤维由聚己内酯(PCL)和聚氧乙烯-聚氧丙烯-聚氧乙烯(Lutrol F127)组成。所制备的植入物呈现出快速的药物释放速率,这促使制备了包含相同配方但带有通过溶剂浇铸制备的附加涂膜的新植入物,该涂膜由PCL和Lutrol F127或PCL和乙烯-醋酸乙烯共聚物(Luwax EVA 3)组成。对植入物进行了表征,并在37℃的磷酸盐缓冲盐水(PBS)中获得了乙酰唑胺的体外释放曲线。含有Luwax EVA 3的涂层植入物中乙酰唑胺的释放曲线比含有Lutrol F127的涂层植入物的情况要慢得多,从而实现了持续释放,并且相对于其他眼部给药系统而言具有创新性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7d01/7919046/026c62199f19/pharmaceutics-13-00260-g001.jpg

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