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作为阿昔洛韦眼部给药可能工具的Eudragit微粒

Eudragit microparticles as a possible tool for ophthalmic administration of acyclovir.

作者信息

Cortesi Rita, Ajanji Sara C Lahm, Sivieri Elisa, Manservigi Marco, Fundueanu Gheorghe, Menegatti Enea, Esposito Elisabetta

机构信息

Department of Pharmaceutical Sciences, University of Ferrara.

出版信息

J Microencapsul. 2007 Aug;24(5):445-56. doi: 10.1080/02652040701374889.

Abstract

This paper describes the production and characterization of polyacrylic polymer (Eudragit RL, RS and NE) microparticles by spray drying method. Microparticles were designed for ophthalmic administration of acyclovir. Microparticle morphology was characterized by optical and electron microscopy. The release kinetics of the drug from microspheres were determined by a dialysis method. The spray drying method described allows the production of microparticles with acceptable encapsulation efficiency and appropriate dimensional characteristics for ophthalmic administration. Release profile data indicate that acyclovir is released from microparticles in a controlled manner. In addition the release pattern of the drug is influenced by the type of Eudragit used for microparticle production. Moreover the plaque reduction efficiency of acyclovir containing microparticles (except for RS/NE microspheres) is comparable to that displayed by the free drug. Finally our results suggest that acyclovir containing microparticles could represent an interesting system for the release of this antiviral drug at the eye site.

摘要

本文描述了通过喷雾干燥法制备聚丙烯酸聚合物(尤特奇RL、RS和NE)微粒及其特性。微粒专为阿昔洛韦的眼部给药而设计。通过光学显微镜和电子显微镜对微粒形态进行了表征。采用透析法测定了药物从微球中的释放动力学。所述喷雾干燥法能够制备出具有可接受包封效率且尺寸特性适合眼部给药的微粒。释放曲线数据表明阿昔洛韦以可控方式从微粒中释放。此外,药物的释放模式受用于制备微粒的尤特奇类型的影响。而且,含阿昔洛韦微粒(除RS/NE微球外)的蚀斑减少效率与游离药物相当。最后,我们的结果表明含阿昔洛韦微粒可能是一种在眼部释放这种抗病毒药物的有趣体系。

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