PDF(Pubmed)
Abstract：
UNASSIGNED: \"Quality by Design\" (QbD) is a novel approach to product development that involves understanding the product and process, as well as the relationship between critical quality attributes (CQA) and critical process parameters (CPP). This study aimed to optimize the gabapentin-loaded solid lipid nanoparticle formulation (GP-SLN) using a QbD approach and evaluate in vitro and ex vivo performance.
UNASSIGNED: The GP-SLN formulation was created using the microemulsion method by combining Gelucire 48/16, Tween 80, and Plurol Oleique CC 497. The Box-Behnken experimental design was adopted to investigate the effects of independent factors on dependent factors. The GP-SLN formulation was assessed based on particle size and distribution, zeta potential, morphology, entrapment efficiency, release kinetics, permeation parameters, stability, and nasal toxicity.
UNASSIGNED: The nanoparticles had a cubical shape with a particle size of 185.3±45.6 nm, a zeta potential of -24±3.53 mV, and an entrapment efficiency of 82.57±4.02%. The particle size and zeta potential of the GP-SLNs remained consistent for 3 months and followed Weibull kinetics with a significantly higher ex vivo permeability (1.7 fold) than a gabapentin solution (GP-SOL). Histopathology studies showed that intranasal administration of the GP-SLN formulation had no harmful effects.
UNASSIGNED: The current study reports the successful development of a GP-SLN formulation using QbD. A sustained release of GP was achieved and its nasal permeability was increased. Solid lipid nanoparticles with optimum particle size and high entrapment efficiency may offer a promising approach for the intranasal delivery of drugs.
UNASSIGNED: The GP-SLN formulation was created using the microemulsion method by combining Gelucire 48/16, Tween 80, and Plurol Oleique CC 497. The Box-Behnken experimental design was adopted to investigate the effects of independent factors on dependent factors. The GP-SLN formulation was assessed based on particle size and distribution, zeta potential, morphology, entrapment efficiency, release kinetics, permeation parameters, stability, and nasal toxicity.
UNASSIGNED: The nanoparticles had a cubical shape with a particle size of 185.3±45.6 nm, a zeta potential of -24±3.53 mV, and an entrapment efficiency of 82.57±4.02%. The particle size and zeta potential of the GP-SLNs remained consistent for 3 months and followed Weibull kinetics with a significantly higher ex vivo permeability (1.7 fold) than a gabapentin solution (GP-SOL). Histopathology studies showed that intranasal administration of the GP-SLN formulation had no harmful effects.
UNASSIGNED: The current study reports the successful development of a GP-SLN formulation using QbD. A sustained release of GP was achieved and its nasal permeability was increased. Solid lipid nanoparticles with optimum particle size and high entrapment efficiency may offer a promising approach for the intranasal delivery of drugs.
摘要：
■“设计质量”（QbD）是一种新颖的产品开发方法，涉及了解产品和工艺，以及关键质量属性(CQA)和关键工艺参数(CPP)之间的关系。本研究旨在使用QbD方法优化加巴喷丁负载的固体脂质纳米颗粒制剂（GP-SLN），并评估体外和离体性能。
■GP-SLN制剂使用微乳液方法通过组合Gelucire48/16、Tween80和PluroolOleiqueCC497来产生。采用Box-Behnken实验设计研究了独立因素对依赖因素的影响。GP-SLN配方基于粒度和分布进行评估，zeta电位,形态学,截留效率，释放动力学，渗透参数，稳定性,和鼻毒性。
■纳米颗粒具有立方体形状，粒径为185.3±45.6nm，zeta电位为-24±3.53mV，包封率为82.57±4.02%。GP-SLN的粒径和ζ电位在3个月内保持一致，并遵循Weibull动力学，其离体渗透性明显高于加巴喷丁溶液（GP-SOL）（1.7倍）。组织病理学研究表明,鼻内施用GP-SLN制剂没有有害作用。
■当前研究报告了使用QbD成功开发GP-SLN制剂。实现了GP的持续释放并增加了其鼻渗透性。具有最佳粒径和高包封效率的固体脂质纳米颗粒可能为药物的鼻内递送提供有希望的方法。
■GP-SLN制剂使用微乳液方法通过组合Gelucire48/16、Tween80和PluroolOleiqueCC497来产生。采用Box-Behnken实验设计研究了独立因素对依赖因素的影响。GP-SLN配方基于粒度和分布进行评估，zeta电位,形态学,截留效率，释放动力学，渗透参数，稳定性,和鼻毒性。
■纳米颗粒具有立方体形状，粒径为185.3±45.6nm，zeta电位为-24±3.53mV，包封率为82.57±4.02%。GP-SLN的粒径和ζ电位在3个月内保持一致，并遵循Weibull动力学，其离体渗透性明显高于加巴喷丁溶液（GP-SOL）（1.7倍）。组织病理学研究表明,鼻内施用GP-SLN制剂没有有害作用。
■当前研究报告了使用QbD成功开发GP-SLN制剂。实现了GP的持续释放并增加了其鼻渗透性。具有最佳粒径和高包封效率的固体脂质纳米颗粒可能为药物的鼻内递送提供有希望的方法。
