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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Development and optimisation of mucoadhesive nanoparticles of acyclovir using design of experiments approach
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Development and optimisation of mucoadhesive nanoparticles of acyclovir using design of experiments approach

机译：使用实验方法开发和优化阿昔洛韦的粘膜粘附纳米颗粒

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摘要

The aim of our study was to improve the bioavailability of acyclovir (ACV) by delivery of mucoadhesive nanoparticles (NPs) and controlled delivery of drug at its absorption window. Central composite design was used by which the effects of independent variables (gelatin and Pluronic F-68) on various responses such as particle size, polydispersity index, entrapment efficiency, loading efficiency, drug release and mucoadhesive strength were studied. The optimised formulation was evaluated for morphology, stability, pharmacokinetic and gastrointestinal tracking. The optimised NPs were found to be nearly spherical. Changes in characteristics of NPs were not significant after six months of accelerated stability studies. In vivo mucoadhesion study showed significant retention of mucoadhesive NPs in upper gastrointestinal tract for more than 12 h. Pharmacokinetic study in rats revealed that mucoadhesive NPs could maintain relatively steady plasma concentration of ACV for more than 10 h. The AUC0-1 and mean residence time of optimised formulation (7527.9 ng h/mL and 12.09 h) were significantly high than tablet dispersion (3841.13 ng h/mL and 7.97 h).
机译：我们研究的目的是通过粘膜粘附纳米颗粒（NPs）的递送和在吸收窗口控制药物的递送来提高阿昔洛韦（ACV）的生物利用度。使用中央复合设计，研究了独立变量（明胶和Pluronic F-68）对各种响应（如粒径，多分散指数，包封率，载药率，药物释放和粘膜黏附强度）的影响。评价了优化的制剂的形态，稳定性，药代动力学和胃肠道追踪。发现优化的NP几乎是球形的。经过六个月的加速稳定性研究，NPs的特征变化不明显。体内粘膜粘附研究显示，粘膜粘附性NP在上消化道中的保留时间超过12小时。在大鼠体内进行的药代动力学研究表明，粘膜粘附性NP可以使ACV的血浆浓度保持相对稳定的时间超过10小时。优化制剂的AUC0-1和平均停留时间（7527.9 ng h / mL和12.09 h）显着高于片剂分散液（3841.13 ng h / mL和7.97 h）。

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