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基于壳聚糖/羟丙基甲基纤维素和聚乙烯吡咯烷酮/羟丙基甲基纤维素聚合物共混物的用于庆大霉素给药的透皮贴剂。

Transdermal patches based on chitosan/hydroxypropyl methylcellulose and polyvinylpyrrolidone/hydroxypropyl methylcellulose polymer blends for gentamycin administration.

作者信息

Jaber Saif Aldeen

机构信息

Faculty of Pharmacy, Middle East University, Amman, Jordan.

Applied Science Research Center, Applied Science Private University, Amman, Jordan.

出版信息

J Adv Pharm Technol Res. 2023 Jul-Sep;14(3):202-207. doi: 10.4103/japtr.japtr_130_23. Epub 2023 Jul 28.

Abstract

Biofilm-forming bacteria have sent alarms to the world about the emerging of bacterial resistance. Gentamycin is an aminoglycoside broad-spectrum antibiotic used against microbial infections. The transdermal drug delivery method is a major system used to reduce drug toxicity and avoid first-pass metabolism. Gentamycin was formulated in a transdermal polymeric formula using hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP), and Chitosan in the presence of palmitic acid as a permeation enhancer. In this research, gentamycin extended drug release behavior was successfully done in different polymeric formulas containing (HPMC/PVP) and (HPMC/Chitosan), with a maximum drug release of <70%. In addition, drug diffusion was found to be dependent on the rate of drug release. The controlled release formulas selected for antimicrobial assay show that HPMC/Chitosan formulas have successfully inhibited microbial and biofilm growth by 90%. In conclusion, gentamycin can be formulated in a transdermal polymeric film to target skin infection, reduce drug side effects and avoid drug first-pass metabolism.

摘要

形成生物膜的细菌已就细菌耐药性的出现向全世界发出警报。庆大霉素是一种用于对抗微生物感染的氨基糖苷类广谱抗生素。透皮给药方法是一种主要用于降低药物毒性和避免首过代谢的系统。在棕榈酸作为渗透促进剂存在的情况下,使用羟丙基甲基纤维素(HPMC)、聚乙烯吡咯烷酮(PVP)和壳聚糖将庆大霉素制成透皮聚合物配方。在本研究中,庆大霉素在含有(HPMC/PVP)和(HPMC/壳聚糖)的不同聚合物配方中成功实现了延长药物释放行为,最大药物释放率<70%。此外,发现药物扩散取决于药物释放速率。选择用于抗菌测定的控释配方表明,HPMC/壳聚糖配方已成功抑制微生物和生物膜生长达90%。总之,庆大霉素可制成透皮聚合物薄膜,以靶向皮肤感染、减少药物副作用并避免药物首过代谢。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c66b/10483904/d2623ea66ee0/JAPTR-14-202-g002.jpg

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