用于鼻内给药的加巴喷丁固体脂质纳米颗粒的开发和表征的质量设计方法:体外、体内和组织病理学评估。

IF 2.1 4区 医学 Q3 MEDICINE, RESEARCH & EXPERIMENTAL
Mahmut Ozan Toksoy, Fırat Aşır, Mert Can Güzel
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引用次数: 0

摘要

目标:"质量源于设计"(QbD)是一种新颖的产品开发方法,它涉及对产品和工艺的理解,以及关键质量属性(CQA)和关键工艺参数(CPP)之间的关系。本研究旨在采用 QbD 方法优化加巴喷丁固体脂质纳米颗粒配方(GP-SLN),并评估其体外和体内性能:GP-SLN 配方采用微乳液法,将 Gelucire 48/16、Tween 80 和 Plurol Oleique CC 497 混合制成。采用箱-贝肯实验设计来研究独立因素对因果因素的影响。根据粒度和分布、ZETA电位、形态、夹带效率、释放动力学、渗透参数、稳定性和鼻腔毒性对GP-SLN配方进行了评估:纳米颗粒呈立方体,粒径为 185.3±45.6 nm,zeta 电位为 -24±3.53 mV,包埋效率为 82.57±4.02%。GP-SLNs 的粒径和 zeta 电位在 3 个月内保持一致,并遵循 Weibull 动力学,其体内渗透率(1.7 倍)明显高于加巴喷丁溶液(GP-SOL)。组织病理学研究表明,鼻内给药 GP-SLN 制剂不会产生有害影响:本研究报告了利用 QbD 成功开发 GP-SLN 制剂的情况。结论:本研究报告了利用 QbD 成功开发 GP-SLN 制剂的情况,该制剂实现了 GP 的持续释放并提高了其鼻腔渗透性。具有最佳粒径和高包封效率的固体脂质纳米颗粒为鼻内给药提供了一种前景广阔的方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Quality by design approach for development and characterization of gabapentin-loaded solid lipid nanoparticles for intranasal delivery: In vitro, ex vivo, and histopathological evaluation.

Objectives: "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.

Materials and methods: 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.

Results: 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.

Conclusion: 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.

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来源期刊
Iranian Journal of Basic Medical Sciences
Iranian Journal of Basic Medical Sciences MEDICINE, RESEARCH & EXPERIMENTAL-PHARMACOLOGY & PHARMACY
CiteScore
4.00
自引率
4.50%
发文量
142
审稿时长
6-12 weeks
期刊介绍: The Iranian Journal of Basic Medical Sciences (IJBMS) is a peer-reviewed, monthly publication by Mashhad University of Medical Sciences (MUMS), Mashhad, Iran . The Journal of "IJBMS” is a modern forum for scientific communication. Data and information, useful to investigators in any discipline in basic medical sciences mainly including Anatomical Sciences, Biochemistry, Genetics, Immunology, Microbiology, Pathology, Pharmacology, Pharmaceutical Sciences, and Physiology, will be published after they have been peer reviewed. This will also include reviews and multidisciplinary research.
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