Amoxicillin loaded-sorbitan monostearate–alginate microparticles as mucoadhesive delivery system for anti-microbial therapy

E. Onuigbo, C. Ugwu, E. Ezeibe, Ifunanya Frank Mama
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Abstract

Antimicrobial resistance has been a challenge to effective antibiotic delivery. Highly technical approaches that meet therapeutic needs are being studied to improve drug bioavailability. This present work seeks to formulate and characterize amoxicillin - loaded sorbitan monostearate-sodium alginate microparticles as mucoadhesive drug delivery for antimicrobial therapy. Three optimized batches of mucoadhesive sorbitan monostearate-alginate microparticles were characterized for particle size, polydispersity index, encapsulation efficiency, viscosity, and mucoadhesivity. Sensitivity test, FTIR spectroscopy and in-vitro drug release were also performed. The particle sizes were between 457 and 872.3 nm. The mean polydispersity index was about 0.569. The encapsulation efficiencies were above 65 %. The pH, viscosity, shear stress and mucoadhesivity were high and decreased gradually with time. The FTIR showed stability and correlation between the formulations and materials used. Sensitivity test showed high susceptibility between 29.00 and 49.33 mm. The drug release followed mostly first order kinetics with R2 > 0.9. Mucoadhesive sorbitan monostearatealginate polymer can be explored as a novel construct for better delivery of amoxicillin.Keywords: sorbitan monostearate, sodium alginate, mucoadhesion, bioavailability, amoxicillin
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载阿莫西林-山梨糖单硬脂酸-海藻酸盐微颗粒作为抗微生物治疗的黏附输送系统
抗菌素耐药性一直是有效抗生素递送的挑战。正在研究满足治疗需要的高技术方法,以提高药物的生物利用度。目前的工作旨在制定和表征阿莫西林负载山梨糖单硬脂酸-海藻酸钠微颗粒作为抗菌治疗的黏附药物递送。对优化后的三批山梨糖单硬脂酸海藻酸酯微颗粒进行了粒径、多分散指数、包封效率、粘度和粘接性能的表征。并进行了药敏试验、FTIR光谱和体外释药试验。粒径在457 ~ 872.3 nm之间。平均多分散性指数约为0.569。包封效率在65%以上。pH值、黏度、剪切应力和黏附力均较高,且随时间的延长逐渐降低。FTIR显示了配方和所用材料之间的稳定性和相关性。敏感性试验显示,29.00 ~ 49.33 mm间敏感性较高。药物释放主要服从一级动力学,R2 > 0.9。粘接山梨糖单硬脂酸海藻酸酯聚合物可以作为一种新的结构,以更好地传递阿莫西林。关键词:单硬脂酸山梨糖,海藻酸钠,黏附,生物利用度,阿莫西林
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